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Hing Sham

Research Profile

Concepts & Ideas

Chemicals & Drugs

Living Beings

Mouse
Rats

Procedures

Occupations

Drug Design

Genes & Molecular Sequences

Molecular Structure

Anatomy

Microsomes, Liver

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Co-author Network

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Publications

TOP 3
Ying-Zi Xu; Jiangli Yan; Nanhua Yao; Shendong Yuan; Yong L Zhu; Paul Beroza; Michael P Bova; Simeon Bowers; Eric Brecht; Wayman Chan; Roy K Hom; Julie Lougheed; Hu Pan; Zhao Ren; Lany Ruslim; Hing L Sham; Danny Tam; Dean R Artis
Design and synthesis of thiophene dihydroisoquinolines as novel BACE1 inhibitors.
Simeon Bowers; Eric Brecht; Wayman Chan; Roy K Hom; Andrei W Konradi; Julie Lougheed; Hu Pan; Gary D Probst; Zhao Ren; Lany Ruslim; Hing L Sham; Danny Tam; Ying-zi Xu; Nanhua Yao; Shendong Yuan; Yong L Zhu; Paul Beroza; Michael P Bova; Dean R Artis
Structure-based design of novel dihydroisoquinoline BACE-1 inhibitors that do not engage the catalytic aspartates.
Maurizio Franzini; Albert W Garofalo; Shawn Gauby; Erich Goldbach; Gary D Probst; Kevin P Quinn; Pam Santiago; Hing L Sham; Danny Tam; Anh Truong; Xiaocong M Ye; Marc Adler; Danielle L Aubele; Zhao Ren
Triazolopyridazine LRRK2 kinase inhibitors.

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All Publications

2013: Ying-Zi Xu; Jiangli Yan; Nanhua Yao; Shendong Yuan; Yong L Zhu; Paul Beroza; Michael P Bova; Simeon Bowers; Eric Brecht; Wayman Chan; Roy K Hom; Julie Lougheed; Hu Pan; Zhao Ren; Lany Ruslim; Hing L Sham; Danny Tam; Dean R Artis
Design and synthesis of thiophene dihydroisoquinolines as novel BACE1 inhibitors.
Bioorganic & medicinal chemistry letters 2013;23(10):3075-80.
2013: Simeon Bowers; Eric Brecht; Wayman Chan; Roy K Hom; Andrei W Konradi; Julie Lougheed; Hu Pan; Gary D Probst; Zhao Ren; Lany Ruslim; Hing L Sham; Danny Tam; Ying-zi Xu; Nanhua Yao; Shendong Yuan; Yong L Zhu; Paul Beroza; Michael P Bova; Dean R Artis
Structure-based design of novel dihydroisoquinoline BACE-1 inhibitors that do not engage the catalytic aspartates.
Bioorganic & medicinal chemistry letters 2013;23(7):2181-6.
2013: Maurizio Franzini; Albert W Garofalo; Shawn Gauby; Erich Goldbach; Gary D Probst; Kevin P Quinn; Pam Santiago; Hing L Sham; Danny Tam; Anh Truong; Xiaocong M Ye; Marc Adler; Danielle L Aubele; Zhao Ren
Triazolopyridazine LRRK2 kinase inhibitors.
Bioorganic & medicinal chemistry letters 2013;23(7):1967-73.
2013: Albert W Garofalo; Erich Goldbach; Grace T Kwong; Ruth Motter; Gary D Probst; Kevin P Quinn; Marc Adler; Danielle L Aubele; Elizabeth F Brigham; David Chian; Maurizio Franzini; Lany Ruslim; Hing L Sham; Danny Tam; Pearl Tanaka; Anh P Truong; Xiaocong M Ye; Zhao Ren
Discovery of 4-alkylamino-7-aryl-3-cyanoquinoline LRRK2 kinase inhibitors.
Bioorganic & medicinal chemistry letters 2013;23(7):1974-7.
2013: Xiaocong M Ye; Shendong Yuan; Hongbin H Zhang; Danielle L Aubele; Michael Bova; Elizabeth Brigham; Michael Dappen; Darren B Dressen; Albert W Garofalo; Erich Goldbach; Jacek J Jagodzinski; Andrei W Konradi; Grace T Kwong; Lee Latimer; Daniel Ness; Gary D Probst; Kevin P Quinn; John-Michael Sauer; Hing L Sham; Minghua Sun; George Tonn; Chris Willtis; David Wone; Ying-zi Xu; Guriqbal S Basi
Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors.
Bioorganic & medicinal chemistry letters 2013;23(4):996-1000.
2013: Albert W Garofalo; Erich Goldbach; Colin Lorentzen; R Jeffrey Neitz; Gary D Probst; Kevin P Quinn; Marc Adler; Danielle L Aubele; Simeon Bowers; Maurizio Franzini; Pam Santiago; Hing L Sham; Danny Tam; Anh P Truong; Xiaocong M Ye; Zhao Ren
Novel cinnoline-based inhibitors of LRRK2 kinase activity.
Bioorganic & medicinal chemistry letters 2013;23(1):71-4.
2011: Danielle L Aubele; Michael P Bova; Simeon Bowers; Elizabeth F Brigham; Darren B Dressen; Albert W Garofalo; Erich Goldbach; Susanna S Hemphill; Andrei W Konradi; Matthew N Mattson; Lan Nguyen; Gary D Probst; Kevin P Quinn; John-Michael Sauer; Chris M Semko; Hing L Sham; Minghua Sun; Anh P Truong; William Wallace; Karina Wong; Wes Zmolek; Guriqbal S Basi
Design, synthesis and structure-activity relationship of novel [3.3.1] bicyclic sulfonamide-pyrazoles as potent γ-secretase inhibitors.
Bioorganic & medicinal chemistry letters 2011;21(19):5791-4.
2011: R Jeffrey Neitz; Andrei W Konradi; Hing L Sham; Wes Zmolek; Karina Wong; Ann Qin; Colin Lorentzen; David Nakamura; Kevin P Quinn; John-Michael Sauer; Kyle Powell; Lany Ruslim; David Chereau; Zhao Ren; John Anderson; Frédérique Bard; Ted A Yednock; Irene Griswold-Prenner
Highly selective c-Jun N-terminal kinase (JNK) 3 inhibitors with in vitro CNS-like pharmacokinetic properties II. Central core replacement.
Bioorganic & medicinal chemistry letters 2011;21(12):3726-9.
2011: Simeon Bowers; Anh P Truong; R Jeffrey Neitz; Martin Neitzel; Gary D Probst; Roy K Hom; Brian Peterson; Robert Anthony Galemmo; Andrei W Konradi; Hing L Sham; Gergley Tóth; Hu Pan; Nanhua Yao; Dean R Artis; Elizabeth F Brigham; Kevin P Quinn; John-Michael Sauer; Kyle Powell; Lany Ruslim; Zhao Ren; Frédérique Bard; Ted Yednock; Irene Griswold-Prenner
Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor.
Bioorganic & medicinal chemistry letters 2011;21(6):1838-43.
2011: Gary D Probst; Simeon Bowers; Jennifer M Sealy; Anh P Truong; Roy K Hom; Robert Anthony Galemmo; Andrei W Konradi; Hing L Sham; David A Quincy; Hu Pan; Nanhua Yao; May Lin; Gergley Tóth; Dean R Artis; Wes Zmolek; Karina Wong; Ann Qin; Colin Lorentzen; David F Nakamura; Kevin P Quinn; John-Michael Sauer; Kyle Powell; Lany Ruslim; Sarah Wright; David Chereau; Zhao Ren; John P Anderson; Frédérique Bard; Ted A Yednock; Irene Griswold-Prenner
Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration.
Bioorganic & medicinal chemistry letters 2011;21(1):315-9.
2010: Roy K Hom; Simeon Bowers; Jennifer M Sealy; Anh P Truong; Gary D Probst; Martin L Neitzel; R Jeffrey Neitz; Larry Fang; Louis Brogley; Jing Wu; Andrei W Konradi; Hing L Sham; Gergely Tóth; Hu Pan; Nanhua Yao; Dean R Artis; Kevin Quinn; John-Michael Sauer; Kyle Powell; Zhao Ren; Frédérique Bard; Ted A Yednock; Irene Griswold-Prenner
Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK.
Bioorganic & medicinal chemistry letters 2010;20(24):7303-7.
2010: Anh P Truong; Gary D Probst; Jose Aquino; Larry Fang; Louis Brogley; Jennifer M Sealy; Roy K Hom; John A Tucker; Varghese John; jay tung; Michael A Pleiss; Andrei W Konradi; Hing L Sham; Michael S Dappen; Gergley Tóth; Nanhua Yao; Eric Brecht; Hu Pan; Dean R Artis; Lany Ruslim; Michael P Bova; Sukanto Sinha; Ted A Yednock; Wes Zmolek; Kevin P Quinn; John-Michael Sauer
Improving the permeability of the hydroxyethylamine BACE-1 inhibitors: structure-activity relationship of P2' substituents.
Bioorganic & medicinal chemistry letters 2010;20(16):4789-94.
2010: Xiaocong M Ye; Andrei W Konradi; Jenifer Smith; Danielle L Aubele; Albert W Garofalo; Jennifer Marugg; Marty L Neitzel; Chris M Semko; Hing L Sham; Minghua Sun; Anh P Truong; Jing Wu; Hongbin Zhang; Erich Goldbach; John-Michael Sauer; Elizabeth F Brigham; Michael Bova; Guriqbal S Basi
Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious gamma-secretase inhibitors (Part II).
Bioorganic & medicinal chemistry letters 2010;20(12):3502-6.
2010: Jason A Segreti; Kristin A Brooks; Kennan Marsh; Joy L Bauch; Yan Lan; C Thomas Lin; Saul H Rosenberg; Hing L Sham; Glenn A Reinhart; Bryan Cox; James S Polakowski
Tumour-selective antivascular effects of the novel anti-mitotic compound A-318315: An in vivo rat regional haemodynamic study.
Clinical and experimental pharmacology & physiology 2010;37(5-6):636-40.
2010: Xiaocong M Ye; Andrei W Konradi; Jenifer Smith; Ying-Zi Xu; Darren Dressen; Albert W Garofalo; Jennifer Marugg; Hing L Sham; Anh P Truong; Jacek Jagodzinski; Michael Pleiss; Hongbin Zhang; Erich Goldbach; John-Michael Sauer; Elizabeth Brigham; Michael Bova; Guriqbal S Basi
Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious gamma-secretase inhibitors.
Bioorganic & medicinal chemistry letters 2010;20(7):2195-9.
2010: Matthew N Mattson; Martin L Neitzel; David A Quincy; Christopher M Semko; Albert W Garofalo; Pamela S Keim; Andrei W Konradi; Michael A Pleiss; Hing L Sham; Elizabeth F Brigham; Erich G Goldbach; Hongbin Zhang; John-Michael Sauer; Guriqbal S Basi
Discovery of sulfonamide-pyrazole gamma-secretase inhibitors.
Bioorganic & medicinal chemistry letters 2010;20(7):2148-50.
2009: Simeon Bowers; Gary D Probst; Anh P Truong; Roy K Hom; Andrei W Konradi; Hing L Sham; Albert W Garofalo; Karina Wong; Erich Goldbach; Kevin P Quinn; John-Michael Sauer; William Wallace; Lan Nguyen; Susanna S Hemphill; Michael P Bova; Guriqbal S Basi
N-Bridged bicyclic sulfonamides as inhibitors of gamma-secretase.
Bioorganic & medicinal chemistry letters 2009;19(24):6952-6.
2009: Anh P Truong; Danielle L Aubele; Gary D Probst; Martin L Neitzel; Chris M Semko; Simeon Bowers; Darren Dressen; Roy K Hom; Andrei W Konradi; Hing L Sham; Albert W Garofalo; Pamela S Keim; Jing Wu; Michael S Dappen; Karina Wong; Erich Goldbach; Kevin P Quinn; John-Michael Sauer; Elizabeth F Brigham; William Wallace; Lan Nguyen; Susanna S Hemphill; Michael P Bova; Frédérique Bard; Ted A Yednock; Guriqbal Basi
Design, synthesis, and structure-activity relationship of novel orally efficacious pyrazole/sulfonamide based dihydroquinoline gamma-secretase inhibitors.
Bioorganic & medicinal chemistry letters 2009;19(17):4920-3.
2008: Zhili Xin; Hongyu Zhao; Michael D Serby; Bo Liu; Mei Liu; Bruce G Szczepankiewicz; Lissa T J Nelson; Harriet T Smith; Tom S Suhar; Richard S Janis; Ning Cao; Heidi S Camp; Christine A Collins; Hing L Sham; Teresa K Surowy; Gang Liu
Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors.
Bioorganic & medicinal chemistry letters 2008;18(15):4298-302.
2008: Gang Zhao; Andrew J Souers; Martin Voorbach; H Douglas Falls; Brian A Droz; Sevan Brodjian; Yau Yi Lau; Rajesh R Iyengar; Ju Gao; Andrew S Judd; Seble H Wagaw; Matthew M Ravn; Kenneth M Engstrom; John K Lynch; Mathew M Mulhern; Jennifer Freeman; Brian D Dayton; Xiaojun Wang; Nelson Grihalde; Dennis Fry; David W A Beno; Kennan Marsh; Zhi Su; Gilbert J Diaz; Christine A Collins; Hing L Sham; Regina M Reilly; Michael E Brune; Philip R Kym
Validation of diacyl glycerolacyltransferase I as a novel target for the treatment of obesity and dyslipidemia using a potent and selective small molecule inhibitor.
Journal of medicinal chemistry 2008;51(3):380-3.
2007: Zhi-Fu Tao; Gaoquan Li; Yunsong Tong; Kent D Stewart; Zehan Chen; Mai-Ha Bui; Philip J Merta; Chang Park; Peter Kovar; Haiying Zhang; Hing L Sham; Saul H Rosenberg; Thomas J Sowin; Nan-Horng Lin
Discovery of 4'-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-benzonitriles and 4'-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-pyridine-2'-carbonitriles as potent checkpoint kinase 1 (Chk1) inhibitors.
Bioorganic & medicinal chemistry letters 2007;17(21):5944-51.
2007: Yunsong Tong; Magdalena Przytulinska; Zhi-Fu Tao; Jennifer J Bouska; Kent D Stewart; Chang Park; Gaoquan Li; Akiyo Claiborne; Peter Kovar; Zehan Chen; Philip J Merta; Mai-Ha Bui; Amanda Olson; Donald J Osterling; Haiying Zhang; Hing L Sham; Saul H Rosenberg; Thomas J Sowin; Nan-Horng Lin
Cyanopyridyl containing 1,4-dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: improving oral biovailability.
Bioorganic & medicinal chemistry letters 2007;17(20):5665-70.
2007: Le Wang; Gerard M Sullivan; Laura A Hexamer; Lisa Hasvold; Reema Thalji; Magdalena Przytulinska; Zhi-Fu Tao; Gaoquan Li; Zehan Chen; Zhan Xiao; Wen-Zhen Gu; John Xue; Mai-Ha Bui; Philip J Merta; Peter Kovar; Jennifer J Bouska; Haiying Zhang; Chang Park; Kent D Stewart; Hing L Sham; Thomas J Sowin; Saul H Rosenberg; Nan-Horng Lin
Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors.
Journal of medicinal chemistry 2007;50(17):4162-76.
2007: Zhi-Fu Tao; Gaoquan Li; Yunsong Tong; Zehan Chen; Philip J Merta; Peter Kovar; Haiying Zhang; Saul H Rosenberg; Hing L Sham; Thomas J Sowin; Nan-Horng Lin
Synthesis and biological evaluation of 4'-(6,7-disubstituted-2,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-biphenyl-4-ol as potent Chk1 inhibitors.
Bioorganic & medicinal chemistry letters 2007;17(15):4308-15.
2007: Yunsong Tong; Akiyo Claiborne; Magdalena Pyzytulinska; Zhi-Fu Tao; Kent D Stewart; Peter Kovar; Zehan Chen; Robert B Credo; Ran Guan; Philip J Merta; Haiying Zhang; Jennifer J Bouska; Elizabeth A Everitt; Bernard P Murry; Dean Hickman; Tim J Stratton; Jian Wu; Saul H Rosenberg; Hing L Sham; Thomas J Sowin; Nan-Horng Lin
1,4-Dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: extended exploration on phenyl ring substitutions and preliminary ADME/PK studies.
Bioorganic & medicinal chemistry letters 2007;17(13):3618-23.
2007: Gang Liu; John K Lynch; Jennifer Freeman; Bo Liu; Zhili Xin; Hongyu Zhao; Michael D Serby; Philip R Kym; Tom S Suhar; Harriet T Smith; Ning Cao; Ruojing Yang; Richard S Janis; Joel A Krauser; Steven P Cepa; David W A Beno; Hing L Sham; Christine A Collins; Teresa K Surowy; Heidi S Camp
Discovery of potent, selective, orally bioavailable stearoyl-CoA desaturase 1 inhibitors.
Journal of medicinal chemistry 2007;50(13):3086-100.
2007: Gang Zhao; Rajesh R Iyengar; Andrew S Judd; Barbara Cool; William Chiou; Lemma Kifle; Ernst U Frevert; Hing L Sham; Philip R Kym
Discovery and SAR development of thienopyridones: a class of small molecule AMPK activators.
Bioorganic & medicinal chemistry letters 2007;17(12):3254-7.
2007: Hongyu Zhao; Michael D Serby; Harriet T Smith; Ning Cao; Tom S Suhar; Teresa K Surowy; Heidi S Camp; Christine A Collins; Hing L Sham; Gang Liu
Discovery of 1-(4-phenoxypiperidin-1-yl)-2-arylaminoethanone stearoyl-CoA desaturase 1 inhibitors.
Bioorganic & medicinal chemistry letters 2007;17(12):3388-91.
2007: Zhonghua Pei; Xiaofeng Li; Thomas W von Geldern; Kenton Longenecker; Daisy Pireh; Kent D Stewart; Bradley J Backes; Chunqiu Lai; Thomas H Lubben; Stephen J Ballaron; David W A Beno; Anita J Kempf-Grote; Hing L Sham; James M Trevillyan
Discovery and structure-activity relationships of piperidinone- and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV inhibitors.
Journal of medicinal chemistry 2007;50(8):1983-7.
2007: Andrew S Judd; Andrew J Souers; Dariusz Wodka; Gang Zhao; Mathew M Mulhern; Rajesh R Iyengar; Ju Gao; John K Lynch; Jennifer C Freeman; H Douglas Falls; Sevan Brodjian; Brian D Dayton; Regina M Reilly; Gary Gintant; James T Limberis; Ann Mikhail; Sandra T Leitza; Kathryn A Houseman; Gilbert Diaz; Eugene N Bush; Robin Shapiro; Victoria Knourek-Segel; Lisa E Hernandez; Kennan Marsh; Hing L Sham; Christine A Collins; Philip R Kym
Identification of diamino chromone-2-carboxamides as MCHr1 antagonists with minimal hERG channel activity.
Bioorganic & medicinal chemistry letters 2007;17(8):2365-71.
2007: Yunsong Tong; Akiyo Claiborne; Kent D Stewart; Chang Park; Peter Kovar; Zehan Chen; Robert B Credo; Wen-Zhen Gu; Stephen L Gwaltney; Russell A Judge; Haiying Zhang; Saul H Rosenberg; Hing L Sham; Thomas J Sowin; Nan-Horng Lin
Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors.
Bioorganic & medicinal chemistry 2007;15(7):2759-67.
2007: Bradley J Backes; Kenton Longenecker; Gregory L Hamilton; Kent Stewart; Chunqiu Lai; Hana Kopecka; Thomas W von Geldern; David J Madar; Zhonghua Pei; Thomas H Lubben; Bradley A Zinker; Zhenping Tian; Stephen J Ballaron; Michael Stashko; Amanda K Mika; David W A Beno; Anita J Kempf-Grote; Candace Black-Schaefer; Hing L Sham; James M Trevillyan
Pyrrolidine-constrained phenethylamines: The design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibitors from a lead-like screening hit.
Bioorganic & medicinal chemistry letters 2007;17(7):2005-12.
2007: Richard F Clark; Tianyuan Zhang; Xiaojun Wang; Rongqi Wang; Xiaolin Zhang; Heidi S Camp; Bruce A Beutel; Hing L Sham; Yu Gui Gu
Phenoxy thiazole derivatives as potent and selective acetyl-CoA carboxylase 2 inhibitors: Modulation of isozyme selectivity by incorporation of phenyl ring substituents.
Bioorganic & medicinal chemistry letters 2007;17(7):1961-5.
2007: Xiangdong Xu; Moshe Weitzberg; Robert F Keyes; Qun Li; Rongqi Wang; Xiaojun Wang; Xiaolin Zhang; Ernst U Frevert; Heidi S Camp; Bruce A Beutel; Hing L Sham; Yu Gui Gu
The synthesis and structure-activity relationship studies of selective acetyl-CoA carboxylase inhibitors containing 4-(thiazol-5-yl)but-3-yn-2-amino motif: polar region modifications.
Bioorganic & medicinal chemistry letters 2007;17(6):1803-7.
2007: Yu Gui Gu; Moshe Weitzberg; Richard F Clark; Xiangdong Xu; Qun Li; Nathan L Lubbers; Yi Yang; David W A Beno; Deborah L Widomski; Tianyuan Zhang; T Matthew Hansen; Robert F Keyes; Jeffrey F Waring; Sherry L Carroll; Xiaojun Wang; Rongqi Wang; Christine H Healan-Greenberg; Eric A G Blomme; Bruce A Beutel; Hing L Sham; Heidi S Camp
N-{3-[2-(4-alkoxyphenoxy)thiazol-5-yl]-1-methylprop-2-ynyl}carboxy derivatives as acetyl-coA carboxylase inhibitors--improvement of cardiovascular and neurological liabilities via structural modifications.
Journal of medicinal chemistry 2007;50(5):1078-82.
2007: Rajesh R Iyengar; John K Lynch; Mathew M Mulhern; Andrew S Judd; Jennifer C Freeman; Ju Gao; Andrew J Souers; Gang Zhao; Dariusz Wodka; H Doug Falls; Sevan Brodjian; Brian D Dayton; Regina M Reilly; Sue Swanson; Zhi Su; Ruth L Martin; Sandra T Leitza; Kathryn A Houseman; Gilbert Diaz; Christine A Collins; Hing L Sham; Philip R Kym
An evaluation of 3,4-methylenedioxy phenyl replacements in the aminopiperidine chromone class of MCHr1 antagonists.
Bioorganic & medicinal chemistry letters 2007;17(4):874-8.
2007: Andrew J Souers; Rajesh R Iyengar; Andrew S Judd; David W A Beno; Ju Gao; Gang Zhao; Michael E Brune; James J Napier; Mathew M Mulhern; John K Lynch; Jennifer C Freeman; Dariusz Wodka; Chong J Chen; H Douglas Falls; Sevan Brodjian; Brian D Dayton; Gilbert J Diaz; Eugene N Bush; Robin Shapiro; Brian A Droz; Victoria Knourek-Segel; Lisa E Hernandez; Kennan Marsh; Regina M Reilly; Hing L Sham; Christine A Collins; Philip R Kym
Constrained 7-fluorocarboxychromone-4-aminopiperidine based Melanin-concentrating hormone receptor 1 antagonists: the effects of chirality on substituted indan-1-ylamines.
Bioorganic & medicinal chemistry letters 2007;17(4):884-9.
2007: Jyoti R Patel; Qi Shuai; Jurgen Dinges; Martin Winn; Marina Pliushchev; Steven Fung; Katina Monzon; William Chiou; Jiahong Wang; Liping Pan; Seble H Wagaw; Kenneth M Engstrom; Francis A Kerdesky; Kenton Longenecker; Russell A Judge; Wenying Qin; Hovis Imade; Deanne Stolarik; David W A Beno; Michael Brune; Linda E Chovan; Hing L Sham; Peer Jacobson; James T Link
Discovery of adamantane ethers as inhibitors of 11beta-HSD-1: Synthesis and biological evaluation.
Bioorganic & medicinal chemistry letters 2007;17(3):750-5.
2007: Mei Liu; Sanyi Wang; Jill E Clampit; Rebecca J Gum; Deanna L Haasch; cristina Rondinone; James M Trevillyan; Cele Abad-Zapatero; Elizabeth H Fry; Hing L Sham; Gang Liu
Discovery of a new class of 4-anilinopyrimidines as potent c-Jun N-terminal kinase inhibitors: Synthesis and SAR studies.
Bioorganic & medicinal chemistry letters 2007;17(3):668-72.
2007: Gang Liu; Hongyu Zhao; Bo Liu; Zhili Xin; Mei Liu; Michael D Serby; Nathan L Lubbers; Deborah L Widomski; James S Polakowski; David W A Beno; James M Trevillyan; Hing L Sham
Hemodynamic effects of potent and selective JNK inhibitors in anesthetized rats: implication for targeting protein kinases in metabolic diseases.
Bioorganic & medicinal chemistry letters 2007;17(2):495-500.
2007: Jeffrey J Rohde; Marina Pliushchev; Bryan K Sorensen; Dariusz Wodka; Qi Shuai; Jiahong Wang; Steven Fung; Katina Monzon; William J Chiou; Liping Pan; Xiaoqing Deng; Linda E Chovan; Atul Ramaiya; Mark Mullally; Rodger F Henry; Deanne Stolarik; Hovis Imade; Kennan Marsh; David W A Beno; Thomas A Fey; Brian A Droz; Michael E Brune; Heidi S Camp; Hing L Sham; Ernst U Frevert; Peer B Jacobson; James T Link
Discovery and metabolic stabilization of potent and selective 2-amino-N-(adamant-2-yl) acetamide 11beta-hydroxysteroid dehydrogenase type 1 inhibitors.
Journal of medicinal chemistry 2007;50(1):149-64.
2006: Zehan Chen; Zhan Xiao; Wen-Zhen Gu; John Xue; Mai-Ha Bui; Peter Kovar; Gaoquan Li; Gary Wang; Zhi-Fu Tao; Yunsong Tong; Nan-Horng Lin; Hing L Sham; Jean Y J Wang; Thomas J Sowin; Saul H Rosenberg; Haiying Zhang
Selective Chk1 inhibitors differentially sensitize p53-deficient cancer cells to cancer therapeutics.
International journal of cancer. Journal international du cancer 2006;119(12):2784-94.
2006: Ravi Kurukulasuriya; Jeffrey J Rohde; Bruce G Szczepankiewicz; Fatima Basha; Chunqiu Lai; Hwan-Soo Jae; Martin Winn; Kent D Stewart; Kenton Longenecker; Thomas W Lubben; Stephen J Ballaron; Hing L Sham; Thomas W von Geldern
Xanthine mimetics as potent dipeptidyl peptidase IV inhibitors.
Bioorganic & medicinal chemistry letters 2006;16(24):6226-30.
2006: Steven Richards; Bryan K Sorensen; Hwan-Soo Jae; Martin Winn; Yixian Chen; Jiahong Wang; Steven Fung; Katina Monzon; Ernst U Frevert; Peer Jacobson; Hing L Sham; James T Link
Discovery of potent and selective inhibitors of 11beta-HSD1 for the treatment of metabolic syndrome.
Bioorganic & medicinal chemistry letters 2006;16(24):6241-5.
2006: Richard F Clark; Tianyuan Zhang; Zhili Xin; Gang Liu; Ying Wang; T Matthew Hansen; Xiaojun Wang; Rongqi Wang; Xiaolin Zhang; Ernst U Frevert; Heidi S Camp; Bruce A Beutel; Hing L Sham; Yu Gui Gu
Structure-activity relationships for a novel series of thiazolyl phenyl ether derivatives exhibiting potent and selective acetyl-CoA carboxylase 2 inhibitory activity.
Bioorganic & medicinal chemistry letters 2006;16(23):6078-81.
2006: Gang Liu; Hongyu Zhao; Bo Liu; Zhili Xin; Mei Liu; Christi Kosogof; Bruce G Szczepankiewicz; Sanyi Wang; Jill E Clampit; Rebecca J Gum; Deanna L Haasch; James M Trevillyan; Hing L Sham
Aminopyridine carboxamides as c-Jun N-terminal kinase inhibitors: targeting the gatekeeper residue and beyond.
Bioorganic & medicinal chemistry letters 2006;16(22):5723-30.
2006: Zhonghua Pei; Xiaofeng Li; Thomas W von Geldern; David J Madar; Kenton Longenecker; Hong Yong; Thomas H Lubben; Kent D Stewart; Bradley A Zinker; Bradley J Backes; Andrew S Judd; Mathew M Mulhern; Stephen J Ballaron; Michael Stashko; Amanda K Mika; David W A Beno; Glenn A Reinhart; Ryan M Fryer; Lee C Preusser; Anita J Kempf-Grote; Hing L Sham; James M Trevillyan
Discovery of ((4R,5S)-5-amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Journal of medicinal chemistry 2006;49(22):6439-42.
2006: Vince S C Yeh; Jyoti R Patel; Hong Yong; Ravi Kurukulasuriya; Steven Fung; Katina Monzon; William Chiou; Jiahong Wang; Deanne Stolarik; Hovis Imade; David W A Beno; Michael Brune; Peer Jacobson; Hing L Sham; James T Link
Synthesis and biological evaluation of heterocycle containing adamantane 11beta-HSD1 inhibitors.
Bioorganic & medicinal chemistry letters 2006;16(20):5414-9.
2006: Vince S C Yeh; Ravi Kurukulasuriya; David J Madar; Jyoti R Patel; Steven Fung; Katina Monzon; William Chiou; Jiahong Wang; Peer Jacobson; Hing L Sham; James T Link
Synthesis and structural activity relationship of 11beta-HSD1 inhibitors with novel adamantane replacements.
Bioorganic & medicinal chemistry letters 2006;16(20):5408-13.
2006: Zhili Xin; Michael D Serby; Hongyu Zhao; Christi Kosogof; Bruce G Szczepankiewicz; Mei Liu; Bo Liu; Charles W Hutchins; Kathy A Sarris; Ethan D Hoff; H Douglas Falls; Chun W Lin; Christopher A Ogiela; Christine A Collins; Michael E Brune; Eugene N Bush; Brian A Droz; Thomas A Fey; Victoria Knourek-Segel; Robin Shapiro; Peer B Jacobson; David W A Beno; Teresa M Turner; Hing L Sham; Gang Liu
Discovery and pharmacological evaluation of growth hormone secretagogue receptor antagonists.
Journal of medicinal chemistry 2006;49(15):4459-69.
2006: Hongyu Zhao; Michael D Serby; Zhili Xin; Bruce G Szczepankiewicz; Mei Liu; Christi Kosogof; Bo Liu; Lissa T J Nelson; Eric F Johnson; Sanyi Wang; Terry Pederson; Rebecca J Gum; Jill E Clampit; Deanna L Haasch; Cele Abad-Zapatero; Elizabeth H Fry; cristina Rondinone; James M Trevillyan; Hing L Sham; Gang Liu
Discovery of potent, highly selective, and orally bioavailable pyridine carboxamide c-Jun NH2-terminal kinase inhibitors.
Journal of medicinal chemistry 2006;49(15):4455-8.
2006: Yu Gui Gu; Moshe Weitzberg; Richard F Clark; Xiangdong Xu; Qun Li; Tianyuan Zhang; T Matthew Hansen; Gang Liu; Zhili Xin; Xiaojun Wang; Rongqi Wang; Teresa McNally; Bradley A Zinker; Ernst U Frevert; Heidi S Camp; Heidi Camp; Bruce A Beutel; Hing L Sham
Synthesis and structure-activity relationships of N-{3-[2-(4-alkoxyphenoxy)thiazol-5-yl]-1- methylprop-2-ynyl}carboxy derivatives as selective acetyl-CoA carboxylase 2 inhibitors.
Journal of medicinal chemistry 2006;49(13):3770-3.
2006: Bruce G Szczepankiewicz; Christi Kosogof; Lissa T J Nelson; Gang Liu; Bo Liu; Hongyu Zhao; Michael D Serby; Zhili Xin; Mei Liu; Rebecca J Gum; Deanna L Haasch; Sanyi Wang; Jill E Clampit; Eric F Johnson; Thomas H Lubben; Michael Stashko; Edward T Olejniczak; Chaohong Sun; Sarah A Dorwin; Kristi Haskins; Cele Abad-Zapatero; Elizabeth H Fry; Charles W Hutchins; Hing L Sham; cristina Rondinone; James M Trevillyan
Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity.
Journal of medicinal chemistry 2006;49(12):3563-80.
2006: Zhonghua Pei; Xiaofeng Li; Kenton Longenecker; Thomas W von Geldern; Paul E Wiedeman; Thomas H Lubben; Bradley A Zinker; Kent Stewart; Stephen J Ballaron; Michael Stashko; Amanda K Mika; David W A Beno; Michelle Long; Heidi Wells; Anita J Kempf-Grote; David J Madar; Todd S McDermott; Lakshmi Bhagavatula; Michael G Fickes; Daisy Pireh; Larry R Solomon; Marc R Lake; Rohinton Edalji; Elizabeth H Fry; Hing L Sham; James M Trevillyan
Discovery, structure-activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase IV inhibitors.
Journal of medicinal chemistry 2006;49(12):3520-35.
2006: Mei Liu; Zhili Xin; Jill E Clampit; Sanyi Wang; Rebecca J Gum; Deanna L Haasch; James M Trevillyan; Cele Abad-Zapatero; Elizabeth H Fry; Hing L Sham; Gang Liu
Synthesis and SAR of 1,9-dihydro-9-hydroxypyrazolo[3,4-b]quinolin-4-ones as novel, selective c-Jun N-terminal kinase inhibitors.
Bioorganic & medicinal chemistry letters 2006;16(10):2590-4.
2006: Michael D Serby; Hongyu Zhao; Bruce G Szczepankiewicz; Christi Kosogof; Zhili Xin; Bo Liu; Mei Liu; Lissa T J Nelson; Wiweka Kaszubska; H Douglas Falls; Verlyn G Schaefer; Eugene N Bush; Robin Shapiro; Brian A Droz; Victoria Knourek-Segel; Thomas A Fey; Michael E Brune; David W A Beno; Theresa M Turner; Christine A Collins; Peer B Jacobson; Hing L Sham; Gang Liu
2,4-diaminopyrimidine derivatives as potent growth hormone secretagogue receptor antagonists.
Journal of medicinal chemistry 2006;49(8):2568-78.
2006: Gaoquan Li; Lisa Hasvold; Zhi-Fu Tao; Gary T Wang; Stephen L Gwaltney; Jyoti Patel; Peter Kovar; Robert B Credo; Zehan Chen; Haiying Zhang; Chang Park; Hing L Sham; Thomas J Sowin; Saul H Rosenberg; Nan-Horng Lin
Synthesis and biological evaluation of 1-(2,4,5-trisubstituted phenyl)-3-(5-cyanopyrazin-2-yl)ureas as potent Chk1 kinase inhibitors.
Bioorganic & medicinal chemistry letters 2006;16(8):2293-8.
2006: Philip R Kym; Andrew J Souers; Thomas J Campbell; John K Lynch; Andrew S Judd; Rajesh R Iyengar; Anil Vasudevan; Ju Gao; Jennifer C Freeman; Dariusz Wodka; Mathew M Mulhern; Gang Zhao; Seble H Wagaw; James J Napier; Sevan Brodjian; Brian D Dayton; Regina M Reilly; Jason A Segreti; Ryan M Fryer; Lee C Preusser; Glenn A Reinhart; Lisa Hernandez; Kennan Marsh; Hing L Sham; Christine A Collins; James S Polakowski
Screening for cardiovascular safety: a structure-activity approach for guiding lead selection of melanin concentrating hormone receptor 1 antagonists.
Journal of medicinal chemistry 2006;49(7):2339-52.
2006: Bo Liu; Mei Liu; Zhili Xin; Hongyu Zhao; Michael D Serby; Christi Kosogof; Lissa T J Nelson; Bruce G Szczepankiewicz; Wiweka Kaszubska; Verlyn G Schaefer; H Douglas Falls; Chun W Lin; Christine A Collins; Hing L Sham; Gang Liu
Optimization of 2,4-diaminopyrimidines as GHS-R antagonists: side chain exploration.
Bioorganic & medicinal chemistry letters 2006;16(7):1864-8.
2006: Nan-Horng Lin; Ping Xia; Peter Kovar; Chang Park; Zehan Chen; Haiying Zhang; Saul H Rosenberg; Hing L Sham
Synthesis and biological evaluation of 3-ethylidene-1,3-dihydro-indol-2-ones as novel checkpoint 1 inhibitors.
Bioorganic & medicinal chemistry letters 2006;16(2):421-6.
2005: Chen Zhao; Hing L Sham; Minghua Sun; Vincent S Stoll; Kent D Stewart; Shuqun Lin; Hongmei Mo; Sudthida Vasavanonda; Ayda Saldivar; Chang Park; Edith J McDonald; Kennan Marsh; Larry Klein; Dale J Kempf; Daniel W Norbeck
Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains.
Bioorganic & medicinal chemistry letters 2005;15(24):5499-503.
2005: Wen-Zhen Gu; Ingrid B J K Joseph; Yi-Chun Wang; David Frost; Gerard M Sullivan; Le Wang; Nan-Horng Lin; Jerry Cohen; Vincent S Stoll; Clarissa Jakob; Steven W Muchmore; John Harlan; Thomas F Holzman; Karl A Walten; Uri S Ladror; Mark G Anderson; Paul Kroeger; Luis E Rodriguez; Ken Jarvis; Debra Ferguson; Kennan Marsh; Shichung Ng; Saul H Rosenberg; Hing L Sham; Haiying Zhang
A highly potent and selective farnesyltransferase inhibitor ABT-100 in preclinical studies.
Anti-cancer drugs 2005;16(10):1059-69.
2005: Anil Vasudevan; Matthew J LaMarche; Christopher Blackburn; Jennifer Lee Che; Courtney A Luchaco-Cullis; Sujen Lai; Thomas H Marsilje; Michael A Patane; Andrew J Souers; Dariusz Wodka; Bradley Geddes; Sumiao Chen; Sevan Brodjian; Doug H Falls; Brian D Dayton; Eugene N Bush; Michael Brune; Robin D Shapiro; Kennan Marsh; Lisa E Hernandez; Hing L Sham; Christine A Collins; Philip R Kym
Identification of ortho-amino benzamides and nicotinamides as MCHr1 antagonists.
Bioorganic & medicinal chemistry letters 2005;15(19):4174-9.
2005: Clarence J Maring; Vincent S Stoll; Chen Zhao; Minghua Sun; Allan C Krueger; Kent D Stewart; Darold L Madigan; Warren M Kati; Yibo Xu; Robert Carrick; Debra A Montgomery; Anita J Kempf-Grote; Kennan Marsh; Akhteruzzaman Molla; Kevin Steffy; Hing L Sham; W Graeme Laver; Yu Gui Gu; Dale J Kempf; William Kohlbrenner
Structure-based characterization and optimization of novel hydrophobic binding interactions in a series of pyrrolidine influenza neuraminidase inhibitors.
Journal of medicinal chemistry 2005;48(12):3980-90.
2005: Qun Li; Tongmei Li; Keith W Woods; Wen-Zhen Gu; Jerry Cohen; Vincent S Stoll; Tomas Galicia; Charles W Hutchins; David Frost; Saul H Rosenberg; Hing L Sham
Benzimidazolones and indoles as non-thiol farnesyltransferase inhibitors based on tipifarnib scaffold: synthesis and activity.
Bioorganic & medicinal chemistry letters 2005;15(11):2918-22.
2005: Andrew J Souers; Ju Gao; Dariusz Wodka; Andrew S Judd; Mathew M Mulhern; James J Napier; Michael E Brune; Eugene N Bush; Sevan Brodjian; Brian D Dayton; Robin Shapiro; Lisa E Hernandez; Kennan Marsh; Hing L Sham; Christine A Collins; Philip R Kym
Synthesis and evaluation of urea-based indazoles as melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity.
Bioorganic & medicinal chemistry letters 2005;15(11):2752-7.
2005: Gary T Wang; Gaoquan Li; Robert A Mantei; Zehan Chen; Peter Kovar; Wendy Gu; Zhan Xiao; Haiying Zhang; Hing L Sham; Thomas J Sowin; Saul H Rosenberg; Nan-Horng Lin
1-(5-Chloro-2-alkoxyphenyl)-3-(5-cyanopyrazin-2-yl)ureas [correction of cyanopyrazi] as potent and selective inhibitors of Chk1 kinase: synthesis, preliminary SAR, and biological activities.
Journal of medicinal chemistry 2005;48(9):3118-21.
2005: Debra Ferguson; Luis E Rodriguez; Joann P Palma; Marion Refici; Ken Jarvis; Jacqueline O'Connor; Gerard M Sullivan; David Frost; Kennan Marsh; Joy Bauch; Haiying Zhang; Nan-Horng Lin; Saul Rosenberg; Hing L Sham; Ingrid B J K Joseph
Antitumor activity of orally bioavailable farnesyltransferase inhibitor, ABT-100, is mediated by antiproliferative, proapoptotic, and antiangiogenic effects in xenograft models.
Clinical cancer research : an official journal of the American Association for Cancer Research 2005;11(8):3045-54.
2005: Qun Li; Keith W Woods; Weibo Wang; Nan-Horng Lin; Akiyo Claiborne; Wen-Zhen Gu; Jerry Cohen; Vincent S Stoll; Charles W Hutchins; David Frost; Saul H Rosenberg; Hing L Sham
Design, synthesis, and activity of achiral analogs of 2-quinolones and indoles as non-thiol farnesyltransferase inhibitors.
Bioorganic & medicinal chemistry letters 2005;15(8):2033-9.
2005: Zehan Chen; Philip J Merta; Nan-Horng Lin; Stephen K Tahir; Peter Kovar; Hing L Sham; Haiying Zhang
A-432411, a novel indolinone compound that disrupts spindle pole formation and inhibits human cancer cell growth.
Molecular cancer therapeutics 2005;4(4):562-8.
2005: Hongyu Zhao; Zhili Xin; Jyoti R Patel; Lissa T J Nelson; Bo Liu; Bruce G Szczepankiewicz; Verlyn G Schaefer; H Douglas Falls; Wiweka Kaszubska; Christine A Collins; Hing L Sham; Gang Liu
Structure-activity relationship studies on tetralin carboxamide growth hormone secretagogue receptor antagonists.
Bioorganic & medicinal chemistry letters 2005;15(7):1825-8.
2005: Andrew J Souers; Ju Gao; Michael Brune; Eugene N Bush; Dariusz Wodka; Anil Vasudevan; Andrew S Judd; Mathew M Mulhern; Sevan Brodjian; Brian D Dayton; Robin Shapiro; Lisa E Hernandez; Kennan Marsh; Hing L Sham; Christine A Collins; Philip R Kym
Identification of 2-(4-benzyloxyphenyl)-N- [1-(2-pyrrolidin-1-yl-ethyl)-1H-indazol-6-yl]acetamide, an orally efficacious melanin-concentrating hormone receptor 1 antagonist for the treatment of obesity.
Journal of medicinal chemistry 2005;48(5):1318-21.
2005: Zhili Xin; Hongyu Zhao; Michael D Serby; Bo Liu; Verlyn G Schaefer; Doug H Falls; Wiweka Kaszubska; Christine A Colins; Hing L Sham; Gang Liu
Synthesis and structure-activity relationships of isoxazole carboxamides as growth hormone secretagogue receptor antagonists.
Bioorganic & medicinal chemistry letters 2005;15(4):1201-4.
2005: Gary T Wang; Xilu Wang; Weibo Wang; Lisa Hasvold; Gerry Sullivan; Charles W Hutchins; Steve O'Conner; Robert Gentiles; Thomas J Sowin; Jerry Cohen; Wen-Zhen Gu; Haiying Zhang; Saul H Rosenberg; Hing L Sham
Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferase.
Bioorganic & medicinal chemistry letters 2005;15(1):153-8.
2004: Hongyu Zhao; Zhili Xin; Gang Liu; Verlyn G Schaefer; H Douglas Falls; Wiweka Kaszubska; Christine A Collins; Hing L Sham
Discovery of tetralin carboxamide growth hormone secretagogue receptor antagonists via scaffold manipulation.
Journal of medicinal chemistry 2004;47(27):6655-7.
2004: Qun Li; Gary T Wang; Tongmei Li; Stephen L Gwaltney; Keith W Woods; Akiyo Claiborne; Xilu Wang; Wendy Gu; Jerry Cohen; Vincent S Stoll; Charles W Hutchins; David Frost; Saul H Rosenberg; Hing L Sham
Synthesis and activity of 1-aryl-1'-imidazolyl methyl ethers as non-thiol farnesyltransferase inhibitors.
Bioorganic & medicinal chemistry letters 2004;14(21):5371-6.
2004: Qun Li; Akiyo Claiborne; Tongmei Li; Lisa Hasvold; Vincent S Stoll; Steven W Muchmore; Clarissa Jakob; Wendy Gu; Jerry Cohen; Charles W Hutchins; David Frost; Saul H Rosenberg; Hing L Sham
Design, synthesis, and activity of 4-quinolone and pyridone compounds as nonthiol-containing farnesyltransferase inhibitors.
Bioorganic & medicinal chemistry letters 2004;14(21):5367-70.
2004: Bo Liu; Gang Liu; Zhili Xin; Michael D Serby; Hongyu Zhao; Verlyn G Schaefer; H Douglas Falls; Wiweka Kaszubska; Christine A Collins; Hing L Sham
Novel isoxazole carboxamides as growth hormone secretagogue receptor (GHS-R) antagonists.
Bioorganic & medicinal chemistry letters 2004;14(20):5223-6.
2004: Nan-Horng Lin; Le Wang; Xilu Wang; Gary T Wang; Jerry Cohen; Wen-Zhen Gu; Haiying Zhang; Saul H Rosenberg; Hing L Sham
Synthesis and biological evaluation of 1-benzyl-5-(3-biphenyl-2-yl-propyl)-1H-imidazole as novel farnesyltransferase inhibitor.
Bioorganic & medicinal chemistry letters 2004;14(20):5057-62.
2004: Le Wang; Nan-Horng Lin; Qun Li; Rodger F Henry; Haiying Zhang; Jerome Cohen; Wen-Zhen Gu; Kennan Marsh; Joy Bauch; Saul H Rosenberg; Hing L Sham
Synthesis of 1H-pyridin-2-one derivatives as potent and selective farnesyltransferase inhibitors.
Bioorganic & medicinal chemistry letters 2004;14(18):4603-6.
2004: Gondi N Kumar; Venkata K Jayanti; Marianne K Johnson; John T Uchic; Samuel Thomas; Ronald D Lee; Brian A Grabowski; Hing L Sham; Dale J Kempf; Jon F Denissen; Kennan Marsh; Eugene Sun; Stanley A Roberts
Metabolism and disposition of the HIV-1 protease inhibitor lopinavir (ABT-378) given in combination with ritonavir in rats, dogs, and humans.
Pharmaceutical research 2004;21(9):1622-30.
2004: Jason A Segreti; James S Polakowski; Kristin A Koch; Kennan Marsh; Joy Bauch; Saul H Rosenberg; Hing L Sham; Bryan Cox; Glenn A Reinhart
Tumor selective antivascular effects of the novel antimitotic compound ABT-751: an in vivo rat regional hemodynamic study.
Cancer chemotherapy and pharmacology 2004;54(3):273-81.
2004: Hing L Sham; David A Betebenner; William Rosenbrook; Thomas Herrin; Ayda Saldivar; Sudthida Vasavanonda; Jacob J Plattner; Daniel W Norbeck
Novel lopinavir analogues incorporating heterocyclic replacements of six-member cyclic urea--synthesis and structure-activity relationships.
Bioorganic & medicinal chemistry letters 2004;14(10):2643-5.
2004: Le Wang; Gary T Wang; Xilu Wang; Yunsong Tong; Gerry Sullivan; David Park; Nicholas M Leonard; Qun Li; Jerry Cohen; Wen-Zhen Gu; Haiying Zhang; Joy Bauch; Clarissa Jakob; Charles W Hutchins; Vincent S Stoll; Kennan Marsh; Saul H Rosenberg; Hing L Sham; Nan-Horng Lin
Design, synthesis, and biological activity of 4-[(4-cyano-2-arylbenzyloxy)-(3-methyl-3H-imidazol-4-yl)methyl]benzonitriles as potent and selective farnesyltransferase inhibitors.
Journal of medicinal chemistry 2004;47(3):612-26.
2003: Lisa Hasvold; Weibo Wang; Stephen L Gwaltney; Todd W Rockway; Lissa T J Nelson; Robert A Mantei; Stephen A Fakhoury; Gerard M Sullivan; Qun Li; Nan-Horng Lin; Le Wang; Haiying Zhang; Jerome Cohen; Wen-Zhen Gu; Kennan Marsh; Joy Bauch; Saul Rosenberg; Hing L Sham
Pyridone-containing farnesyltransferase inhibitors: synthesis and biological evaluation.
Bioorganic & medicinal chemistry letters 2003;13(22):4001-5.
2003: Nan-Horng Lin; Le Wang; Jerry Cohen; Wen-Zhen Gu; David Frost; Haiying Zhang; Saul Rosenberg; Hing L Sham
Synthesis and biological evaluation of 4-[(3-methyl-3H-imidazol-4-yl)-(2-phenylethynyl-benzyloxy)-methyl]-benzonitrile as novel farnesyltransferase inhibitor.
Bioorganic & medicinal chemistry letters 2003;13(21):3821-5.
2003: Xiaoqi Chen; Dale J Kempf; Lin Li; Hing L Sham; Sudthida Vasavanonda; Norman E Wideburg; Ayda Saldivar; Kennan Marsh; Edith McDonald; Daniel W Norbeck
Synthesis and SAR studies of potent HIV protease inhibitors containing novel dimethylphenoxyl acetates as P2 ligands.
Bioorganic & medicinal chemistry letters 2003;13(21):3657-60.
2003: Zehan Chen; Zhan Xiao; Jun Chen; Shi-Chung Ng; Thomas J Sowin; Hing L Sham; Saul Rosenberg; Stephen W Fesik; Haiying Zhang
Human Chk1 expression is dispensable for somatic cell death and critical for sustaining G2 DNA damage checkpoint.
Molecular cancer therapeutics 2003;2(6):543-8.
2003: Yunsong Tong; Nan-Horng Lin; Le Wang; Lisa Hasvold; Weibo Wang; Nicholas Leonard; Tongmei Li; Qun Li; Jerry Cohen; Wen-Zhen Gu; Haiying Zhang; Vincent S Stoll; Joy Bauch; Kennan Marsh; Saul H Rosenberg; Hing L Sham
Discovery of potent imidazole and cyanophenyl containing farnesyltransferase inhibitors with improved oral bioavailability.
Bioorganic & medicinal chemistry letters 2003;13(9):1571-4.
2003: Michael L Curtin; Alan S Florjancic; Jerome Cohen; Wen-Zhen Gu; David Frost; Steven W Muchmore; Hing L Sham
Novel and selective imidazole-containing biphenyl inhibitors of protein farnesyltransferase.
Bioorganic & medicinal chemistry letters 2003;13(7):1367-71.
2003: Stephen L Gwaltney; Stephen J O'Connor; Lissa T J Nelson; Gerard M Sullivan; Hovis Imade; Weibo Wang; Lisa Hasvold; Qun Li; Jerome Cohen; Wen-Zhen Gu; Stephen K Tahir; Joy Bauch; Kennan Marsh; Shi-Chung Ng; David Frost; Haiying Zhang; Steven W Muchmore; Clarissa Jakob; Vincent S Stoll; Charles W Hutchins; Saul H Rosenberg; Hing L Sham
Aryl tetrahydropyridine inhibitors of farnesyltransferase: bioavailable analogues with improved cellular potency.
Bioorganic & medicinal chemistry letters 2003;13(7):1363-6.
2003: Stephen L Gwaltney; Stephen J O'Connor; Lissa T J Nelson; Gerard M Sullivan; Hovis Imade; Weibo Wang; Lisa Hasvold; Qun Li; Jerome Cohen; Wen-Zhen Gu; Stephen K Tahir; Joy Bauch; Kennan Marsh; Shi-Chung Ng; David Frost; Haiying Zhang; Steven W Muchmore; Clarissa Jakob; Vincent S Stoll; Charles W Hutchins; Saul H Rosenberg; Hing L Sham
Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives.
Bioorganic & medicinal chemistry letters 2003;13(7):1359-62.
2003: Nan-Horng Lin; Le Wang; Jerry Cohen; Wen-Zhen Gu; David Frost; Haiying Zhang; Saul Rosenberg; Hing L Sham
Synthesis and biological evaluation of 4-[3-biphenyl-2-yl-1-hydroxy-1-(3-methyl-3H-imidazol-4-yl)-prop-2-ynyl]-1-yl-benzonitrile as novel farnesyltransferase inhibitor.
Bioorganic & medicinal chemistry letters 2003;13(7):1293-6.
2003: Stephen K Tahir; Michael A Nukkala; Nicolette A Zielinski Mozny; Robert B Credo; Robert B Warner; Qun Li; Keith W Woods; Akiyo Claiborne; Stephen L Gwaltney; David Frost; Hing L Sham; Saul H Rosenberg; Shi-Chung Ng
Biological activity of A-289099: an orally active tubulin-binding indolyloxazoline derivative.
Molecular cancer therapeutics 2003;2(3):227-33.
2003: Vincent S Stoll; Kent D Stewart; Clarence J Maring; Steven W Muchmore; Vincent L Giranda; Yu Gui Gu; Gary Wang; Yuanwei Chen; Minghua Sun; Chen Zhao; April L Kennedy; Darold L Madigan; Yibo Xu; Ayda Saldivar; Warren M Kati; Graeme Laver; Thomas J Sowin; Hing L Sham; Jonathan Greer; Dale J Kempf
Influenza neuraminidase inhibitors: structure-based design of a novel inhibitor series.
Biochemistry 2003;42(3):718-27.
2002: Hing L Sham; Chen Zhao; Leping Li; David A Betebenner; Ayda Saldivar; Sudthida Vasavanonda; Dale J Kempf; Jacob J Plattner; Daniel W Norbeck
Novel lopinavir analogues incorporating non-Aromatic P-1 side chains--synthesis and structure--activity relationships.
Bioorganic & medicinal chemistry letters 2002;12(21):3101-3.
2002: Vincent S Stoll; Wenying Qin; Kent D Stewart; Clarissa Jakob; Chang Park; K Walter; Robert L Simmer; Rosalind J Helfrich; Dirk Bussiere; J Kao; Dale J Kempf; Hing L Sham; Daniel W Norbeck
X-ray crystallographic structure of ABT-378 (lopinavir) bound to HIV-1 protease.
Bioorganic & medicinal chemistry 2002;10(8):2803-6.
2002: Hing L Sham; David A Betebenner; Xiaoqi Chen; Ayda Saldivar; Sudthida Vasavanonda; Dale J Kempf; Jacob J Plattner; Daniel W Norbeck
Synthesis and structure-activity relationships of a novel series of HIV-1 protease inhibitors encompassing ABT-378 (Lopinavir).
Bioorganic & medicinal chemistry letters 2002;12(8):1185-7.
2002: Le Wang; Keith W Woods; Qun Li; Kenneth J Barr; Richard W McCroskey; Steven M Hannick; Laura Gherke; Robert B Credo; Yu-Hua Hui; Kennan Marsh; Robert Warner; Jang Y Lee; Nicolette Zielinski-Mozng; David Frost; Saul H Rosenberg; Hing L Sham
Potent, orally active heterocycle-based combretastatin A-4 analogues: synthesis, structure-activity relationship, pharmacokinetics, and in vivo antitumor activity evaluation.
Journal of medicinal chemistry 2002;45(8):1697-711.
2002: Qun Li; Keith W Woods; Akiyo Claiborne; Stephen L Gwaltney; Kenneth J Barr; Gang Liu; Laura Gehrke; Robert B Credo; Yu-Hua Hui; Jang Lee; Robert B Warner; Peter Kovar; Michael A Nukkala; Nicolette A Zielinski; Stephen K Tahir; Michael Fitzgerald; Ki H Kim; Kennan Marsh; David Frost; Shi-Chung Ng; Saul Rosenberg; Hing L Sham
Synthesis and biological evaluation of 2-indolyloxazolines as a new class of tubulin polymerization inhibitors. Discovery of A-289099 as an orally active antitumor agent.
Bioorganic & medicinal chemistry letters 2002;12(3):465-9.
2001: Stephen K Tahir; Edward K Han; B Credo; Hwan-Soo Jae; Jennifer A Pietenpol; CD Scatena; J Ruth Wu-Wong; David Frost; Hing L Sham; Saul H Rosenberg; Shi-Chung Ng
A-204197, a new tubulin-binding agent with antimitotic activity in tumor cell lines resistant to known microtubule inhibitors.
Cancer research 2001;61(14):5480-5.
2001: Stephen L Gwaltney; Hovis Imade; Qun Li; Laura Gehrke; Robert B Credo; Robert B Warner; Jang Y Lee; Peter Kovar; David Frost; Shi-Chung Ng; Hing L Sham
Novel sulfonate derivatives: potent antimitotic agents.
Bioorganic & medicinal chemistry letters 2001;11(13):1671-3.
2001: Hing L Sham; David A Betebenner; T Herrin; G Kumar; Ayda Saldivar; Sudthida Vasavanonda; Akhteruzzaman Molla; Dale J Kempf; Jacob J Plattner; Daniel W Norbeck
Synthesis and antiviral activities of the major metabolites of the HIV protease inhibitor ABT-378 (Lopinavir).
Bioorganic & medicinal chemistry letters 2001;11(11):1351-3.
2001: Gary T Wang; Yuanwei Chen; Sanyi Wang; Robert Gentles; Thomas J Sowin; Warren M Kati; Steven W Muchmore; Vincent L Giranda; Kent Stewart; Hing L Sham; Dale J Kempf; W Graeme Laver
Design, synthesis, and structural analysis of influenza neuraminidase inhibitors containing pyrrolidine cores.
Journal of medicinal chemistry 2001;44(8):1192-201.
2001: Stephen L Gwaltney; Hovis Imade; Kenneth J Barr; Qun Li; Laura Gehrke; Robert B Credo; Robert B Warner; Jang Y Lee; Peter Kovar; Jieyi Wang; Michael A Nukkala; Nicolette A Zielinski; David Frost; Shi-Chung Ng; Hing L Sham
Novel sulfonate analogues of combretastatin A-4: potent antimitotic agents.
Bioorganic & medicinal chemistry letters 2001;11(7):871-4.
2000: Edward K Han; E Kyu-Ho Han; Laura Gehrke; Stephen K Tahir; Robert B Credo; SP Cherian; Hing L Sham; Saul H Rosenberg; Shichung Ng
Modulation of drug resistance by alpha-tubulin in paclitaxel-resistant human lung cancer cell lines.
European journal of cancer (Oxford, England : 1990) 2000;36(12):1565-71.
1999: KJ Henry; JT Wasicak; Andrew Tasker; Jerry Cohen; PJ Ewing; Michael J Mitten; J J Larsen; Douglas Kalvin; R Swenson; Shi-Chung Ng; B Saeed; SP Cherian; Hing L Sham; Saul H Rosenberg
Discovery of a series of cyclohexylethylamine-containing protein farnesyltransferase inhibitors exhibiting potent cellular activity.
Journal of medicinal chemistry 1999;42(23):4844-52.
1999: Stephen J O'Connor; Kenneth J Barr; Le Wang; Bryan K Sorensen; Andrew Tasker; Hing L Sham; Shi-Chung Ng; Jerry Cohen; E Devine; SP Cherian; B Saeed; Haichao Zhang; Jang Y Lee; Robert Warner; Stephen K Tahir; Peter Kovar; PJ Ewing; JD Alder; Michael J Mitten; Juan Leal; Kennan Marsh; Joy Bauch; D J Hoffman; S M Sebti; Saul H Rosenberg
Second-generation peptidomimetic inhibitors of protein farnesyltransferase demonstrating improved cellular potency and significant in vivo efficacy.
Journal of medicinal chemistry 1999;42(18):3701-10.
1999: David J Augeri; David A Janowick; Douglas Kalvin; Gerry Sullivan; J Larsen; Daniel A Dickman; Hong Ding; Jerry Cohen; Jang Lee; Robert Warner; Peter Kovar; SP Cherian; B Saeed; Haichao Zhang; Stephen K Tahir; Shi-Chung Ng; Hing L Sham; Saul H Rosenberg
Potent and orally bioavailable noncysteine-containing inhibitors of protein farnesyltransferase.
Bioorganic & medicinal chemistry letters 1999;9(8):1069-74.
1999: Wang Shen; Stephen A Fakhoury; G Donner; K Henry; Jang Lee; Haichao Zhang; Jerry Cohen; Robert Warner; B Saeed; SP Cherian; Stephen K Tahir; Peter Kovar; Joy Bauch; Shi-Chung Ng; Kennan Marsh; Hing L Sham; Saul Rosenberg
Potent inhibitors of protein farnesyltransferase: heteroarenes as cysteine replacements.
Bioorganic & medicinal chemistry letters 1999;9(5):703-8.
1999: Warren M Kati; Hing L Sham; J Owen McCall; Debra A Montgomery; Gary T Wang; W Rosenbrook; L Miesbauer; Alex M Buko; Daniel W Norbeck
Inhibition of 3C protease from human rhinovirus strain 1B by peptidyl bromomethylketonehydrazides.
Archives of biochemistry and biophysics 1999;362(2):363-75.
1999: Gondi N Kumar; Venkata K Jayanti; R D Lee; D N Whittern; John T Uchic; Samuel Thomas; P Johnson; Brian A Grabowski; Hing L Sham; David A Betebenner; Dale J Kempf; Jon F Denissen
In vitro metabolism of the HIV-1 protease inhibitor ABT-378: species comparison and metabolite identification.
Drug metabolism and disposition: the biological fate of chemicals 1999;27(1):86-91.
1998: Xiaoqi Chen; Dale J Kempf; Hing L Sham; Brian E Green; Akhteruzzaman Molla; M Korneyeva; Sudthida Vasavanonda; Norman E Wideburg; Ayda Saldivar; Kennan Marsh; Edith McDonald; Daniel W Norbeck
Potent piperazine hydroxyethylamine HIV protease inhibitors containing novel P3 ligands.
Bioorganic & medicinal chemistry letters 1998;8(24):3531-6.
1998: Hing L Sham; Dale J Kempf; Akhteruzzaman Molla; Kennan Marsh; Gondi N Kumar; Chih-Ming Chen; Warren M Kati; K Stewart; R Lal; Ann Hsu; David A Betebenner; M Korneyeva; Sudthida Vasavanonda; Edith McDonald; Ayda Saldivar; Norman E Wideburg; Xiaoqi Chen; P Niu; Chang Park; Venkata K Jayanti; Brian A Grabowski; G Richard Granneman; Eugene Sun; Anthony J Japour; JM Leonard; Jacob J Plattner; Daniel W Norbeck
ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease.
Antimicrobial agents and chemotherapy 1998;42(12):3218-24.
1998: Akhteruzzaman Molla; Sudthida Vasavanonda; G Kumar; Hing L Sham; M Johnson; Brian A Grabowski; Jon F Denissen; William Kohlbrenner; Jacob J Plattner; JM Leonard; Daniel W Norbeck; Dale J Kempf
Human serum attenuates the activity of protease inhibitors toward wild-type and mutant human immunodeficiency virus.
Virology 1998;250(2):255-62.
1998: A Carrillo; Kent D Stewart; Hing L Sham; Daniel W Norbeck; William Kohlbrenner; JM Leonard; Dale J Kempf; Akhteruzzaman Molla
In vitro selection and characterization of human immunodeficiency virus type 1 variants with increased resistance to ABT-378, a novel protease inhibitor.
Journal of virology 1998;72(9):7532-41.
1998: Warren M Kati; Ayda Saldivar; F Mohamadi; Hing L Sham; W Graeme Laver; William Kohlbrenner
GS4071 is a slow-binding inhibitor of influenza neuraminidase from both A and B strains.
Biochemical and biophysical research communications 1998;244(2):408-13.
1998: Dale J Kempf; Hing L Sham; Kennan Marsh; Charles A Flentge; David A Betebenner; Brian E Green; Edith McDonald; Sudthida Vasavanonda; Ayda Saldivar; Norman E Wideburg; Warren M Kati; L Ruiz; Chen Zhao; L Fino; J Patterson; Akhteruzzaman Molla; Jacob J Plattner; Daniel W Norbeck
Discovery of ritonavir, a potent inhibitor of HIV protease with high oral bioavailability and clinical efficacy.
Journal of medicinal chemistry 1998;41(4):602-17.
1996: Hing L Sham; C Zhao; Kennan Marsh; David A Betebenner; S Lin; W Rosenbrook; T Herrin; L Li; D Madigan; Sudthida Vasavanonda; Akhteruzzaman Molla; Ayda Saldivar; Edith McDonald; Norman E Wideburg; Dale J Kempf; Daniel W Norbeck; Jacob J Plattner
Novel azacyclic ureas that are potent inhibitors of HIV-1 protease.
Biochemical and biophysical research communications 1996;225(2):436-40.
1996: Hing L Sham; C Zhao; Kent D Stewart; David A Betebenner; S Lin; C H Park; X P Kong; W Rosenbrook; T Herrin; D Madigan; Sudthida Vasavanonda; N Lyons; Akhteruzzaman Molla; Ayda Saldivar; Kennan Marsh; Edith McDonald; Norman E Wideburg; Jon F Denissen; T Robins; Dale J Kempf; Jacob J Plattner; Daniel W Norbeck
A novel, picomolar inhibitor of human immunodeficiency virus type 1 protease.
Journal of medicinal chemistry 1996;39(2):392-7.
1995: Hing L Sham; C Zhao; Kennan Marsh; David A Betebenner; S Lin; Edith McDonald; Sudthida Vasavanonda; Norman E Wideburg; Ayda Saldivar; T Robins
Potent inhibitors of the HIV-1 protease with good oral bioavailabilities.
Biochemical and biophysical research communications 1995;211(1):159-65.
1994: Dale J Kempf; Kennan Marsh; L C Fino; P Bryant; A Craig-Kennard; Hing L Sham; C Zhao; Sudthida Vasavanonda; William Kohlbrenner; Norman E Wideburg
Design of orally bioavailable, symmetry-based inhibitors of HIV protease.
Bioorganic & medicinal chemistry 1994;2(9):847-58.
1993: Hing L Sham; David A Betebenner; Norman E Wideburg; Ayda Saldivar; William Kohlbrenner; A Craig-Kennard; Sudthida Vasavanonda; Dale J Kempf; J J Clement; J E Erickson
Pseudo-symmetrical difluoroketones. Highly potent and specific inhibitors of HIV-1 protease.
FEBS letters 1993;329(1-2):144-6.
1993: Dale J Kempf; L Codacovi; X C Wang; William Kohlbrenner; Norman E Wideburg; Ayda Saldivar; Sudthida Vasavanonda; Kennan Marsh; P Bryant; Hing L Sham
Symmetry-based inhibitors of HIV protease. Structure-activity studies of acylated 2,4-diamino-1,5-diphenyl-3-hydroxypentane and 2,5-diamino-1,6-diphenylhexane-3,4-diol.
Journal of medicinal chemistry 1993;36(3):320-30.
1991: Hing L Sham; David A Betebenner; Norman E Wideburg; Ayda Saldivar; William Kohlbrenner; Sudthida Vasavanonda; Dale J Kempf; Daniel W Norbeck; C Zhao; J J Clement
Potent HIV-1 protease inhibitors with antiviral activities in vitro.
Biochemical and biophysical research communications 1991;175(3):914-9.
1990: Saul H Rosenberg; K W Woods; Hing L Sham; H D Kleinert; D L Martin; H Stein; Jerry Cohen; David A Egan; B Bopp; I Merits
Water-soluble renin inhibitors: design of a subnanomolar inhibitor with a prolonged duration of action.
Journal of medicinal chemistry 1990;33(7):1962-9.
1990: Daniel W Norbeck; E Kern; S Hayashi; W Rosenbrook; Hing L Sham; T Herrin; Jacob J Plattner; J Erickson; J Clement; R Swanson
Cyclobut-A and cyclobut-G: broad-spectrum antiviral agents with potential utility for the therapy of AIDS.
Journal of medicinal chemistry 1990;33(5):1281-5.
1988: Jacob J Plattner; Patrick A Marcotte; H D Kleinert; H H Stein; J Greer; G Bolis; A K Fung; B A Bopp; Jay R Luly; Hing L Sham
Renin inhibitors. Dipeptide analogues of angiotensinogen utilizing a structurally modified phenylalanine residue to impart proteolytic stability.
Journal of medicinal chemistry 1988;31(12):2277-88.
1988: Hing L Sham; G Bolis; H H Stein; Stephen W Fesik; Patrick A Marcotte; Jacob J Plattner; C A Rempel; J Greer
Renin inhibitors. Design and synthesis of a new class of conformationally restricted analogues of angiotensinogen.
Journal of medicinal chemistry 1988;31(2):284-95.
1987: Hing L Sham; H Stein; C A Rempel; J Cohen; Jacob J Plattner
Highly potent and specific inhibitors of human renin.
FEBS letters 1987;220(2):299-301.
1987: S W Fesik; G Bolis; Hing L Sham; E T Olejniczak
Structure refinement of a cyclic peptide from two-dimensional NMR data and molecular modeling.
Biochemistry 1987;26(7):1851-9.
1986: Jacob J Plattner; J Greer; A K Fung; H Stein; H D Kleinert; Hing L Sham; J R Smital; T J Perun
Peptide analogues of angiotensinogen. Effect of peptide chain length on renin inhibition.
Biochemical and biophysical research communications 1986;139(3):982-90.

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