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Mark Norman

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TOP 3
Ryan P Wurz; Kevin Yang; Nancy Zhang; Liping H Pettus; Raju Subramanian; Ling Wang; Douglas A Whittington; Kristin L Andrews; Yunxin Bo; Sean Caenepeel; Daniel J Freeman; Paul E Hughes; Jian Jiang; Longbin Liu; John D McCarter; Tisha San Miguel; Erin L Mullady; Nobuko Nishimura; Mark H Norman
Synthesis and structure-activity relationships of dual PI3K/mTOR inhibitors based on a 4-amino-6-methyl-1,3,5-triazine sulfonamide scaffold.
Mark H Norman; Karen Rex; Ning Xi; Steve Bellon; Noel D D'Angelo; Celia Dominguez; Ingrid Fellows; Tae-Seong Kim; Matthew Lee; Longbin Liu; Isabelle Dussault
Structure-based design of novel class II c-Met inhibitors: 1. Identification of pyrazolone-based derivatives.
Longbin Liu; Mark H Norman; Aaron Siegmund; Douglas A Whittington; Ning Xi; Kevin Yang; Yajing Yang; Yihong Zhang; Steve Bellon; Alessandro A Boezio; Shon Booker; Debbie Choquette; Noel D D'Angelo; Celia Dominguez; Julie Germain; Jean-Christophe Harmange; Tae-Seong Kim; Matthew Lee; Isabelle Dussault
Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.

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All Publications

2012: Ryan P Wurz; Kevin Yang; Nancy Zhang; Liping H Pettus; Raju Subramanian; Ling Wang; Douglas A Whittington; Kristin L Andrews; Yunxin Bo; Sean Caenepeel; Daniel J Freeman; Paul E Hughes; Jian Jiang; Longbin Liu; John D McCarter; Tisha San Miguel; Erin L Mullady; Nobuko Nishimura; Mark H Norman
Synthesis and structure-activity relationships of dual PI3K/mTOR inhibitors based on a 4-amino-6-methyl-1,3,5-triazine sulfonamide scaffold.
Bioorganic & medicinal chemistry letters 2012;22(17):5714-20.
2012: Mark H Norman; Karen Rex; Ning Xi; Steve Bellon; Noel D D'Angelo; Celia Dominguez; Ingrid Fellows; Tae-Seong Kim; Matthew Lee; Longbin Liu; Isabelle Dussault
Structure-based design of novel class II c-Met inhibitors: 1. Identification of pyrazolone-based derivatives.
Journal of medicinal chemistry 2012;55(5):1858-67.
2012: Longbin Liu; Mark H Norman; Aaron Siegmund; Douglas A Whittington; Ning Xi; Kevin Yang; Yajing Yang; Yihong Zhang; Steve Bellon; Alessandro A Boezio; Shon Booker; Debbie Choquette; Noel D D'Angelo; Celia Dominguez; Julie Germain; Jean-Christophe Harmange; Tae-Seong Kim; Matthew Lee; Isabelle Dussault
Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.
Journal of medicinal chemistry 2012;55(5):1868-97.
2012: Nuria A Tamayo; Phi Tang; Weiya Wang; Brad Youngblood; Michael D Bartberger; Yunxin Bo; Jiyun Chen; Tiffany L Correll; Hong Deng; Narender R Gavva; Vijay K Gore; Lana Klionsky; Sonya G Lehto; Vu V Ma; Nobuko Nishimura; Mark H Norman
Fused piperidines as a novel class of potent and orally available transient receptor potential melastatin type 8 (TRPM8) antagonists.
Journal of medicinal chemistry 2012;55(4):1593-611.
2011: Markian M Stec; Raju Subramanian; Nuria A Tamayo; Ling Wang; Kevin Yang; Leeanne P Zalameda; Nancy Zhang; Tisha San Miguel; Kristin L Andrews; Shon K Booker; Sean Caenepeel; Daniel J Freeman; Paul E Hughes; Jian Jiang; Hongyu Liao; John McCarter; Erin L Mullady; Mark H Norman
Structure-activity relationships of phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: investigations of various 6,5-heterocycles to improve metabolic stability.
Journal of medicinal chemistry 2011;54(14):5174-84.
2011: Nobuko Nishimura; Kristin L Andrews; Yunxin Bo; Shon K Booker; Marian C Bryan; Sean Caenepeel; Daniel Freeman; Paul E Hughes; Hongyu Liao; Longbin Liu; John McCarter; Erin L Mullady; Tisha San Miguel; Aaron Siegmund; Raju Subramanian; Nuria A Tamayo; Ling Wang; Douglas A Whittington; Kevin Yang; Leeanne Zalameda; Nancy Zhang; Mark H Norman
Phospshoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: discovery and structure-activity relationships of a series of quinoline and quinoxaline derivatives.
Journal of medicinal chemistry 2011;54(13):4735-51.
2010: Vijay K Gore; Vu V Ma; Ruoyuan Yin; Joe Ligutti; David Immke; Elizabeth M Doherty; Mark H Norman
Structure-activity relationship (SAR) investigations of tetrahydroquinolines as BKCa agonists.
Bioorganic & medicinal chemistry letters 2010;20(12):3573-8.
2008: Markian M Stec; Yunxin Bo; Partha P Chakrabarti; Lillian Liao; Mqhele Ncube; Nuria A Tamayo; Rami Tamir; Narender R Gavva; James J S Treanor; Mark H Norman
Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists.
Bioorganic & medicinal chemistry letters 2008;18(18):5118-22.
2008: Elizabeth M Doherty; Daniel Retz; Narender R Gavva; Rami Tamir; James J S Treanor; Mark H Norman
4-Aminopyrimidine tetrahydronaphthols: a series of novel vanilloid receptor-1 antagonists with improved solubility properties.
Bioorganic & medicinal chemistry letters 2008;18(6):1830-4.
2007: Xianghong Wang; Partha P Chakrabarti; Vassil I Ognyanov; Liping H Pettus; Rami Tamir; Helming Tan; Phi Tang; James J S Treanor; Narender R Gavva; Mark H Norman
Trisubstituted pyrimidines as transient receptor potential vanilloid 1 (TRPV1) antagonists with improved solubility.
Bioorganic & medicinal chemistry letters 2007;17(23):6539-45.
2007: Vellarkad Viswanadhan; Yaxiong Sun; Mark H Norman
Three-dimensional quantitative structure-activity relationships and activity predictions of human TRPV1 channel antagonists: comparative molecular field analysis and comparative molecular similarity index analysis of cinnamides.
Journal of medicinal chemistry 2007;50(23):5608-19.
2007: Vijay K Gore; Vu V Ma; Rami Tamir; Narender R Gavva; James J S Treanor; Mark H Norman
Structure-activity relationship (SAR) investigations of substituted imidazole analogs as TRPV1 antagonists.
Bioorganic & medicinal chemistry letters 2007;17(21):5825-30.
2007: Robert M Rzasa; Matthew R Kaller; Gang Liu; Ella Magal; Thomas T Nguyen; Timothy D Osslund; David Powers; Vincent J Santora; Vellarkad Viswanadhan; Hui-Ling Wang; Xiaoling Xiong; Wenge Zhong; Mark H Norman
Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors.
Bioorganic & medicinal chemistry 2007;15(20):6574-95.
2007: Wenge Zhong; Hu Liu; Matthew R Kaller; Charles Henley; Ella Magal; Thomas Nguyen; Timothy D Osslund; David Powers; Robert M Rzasa; Hui-Ling Wang; Weiya Wang; Xiaoling Xiong; Jiandong Zhang; Mark H Norman
Design and synthesis of quinolin-2(1H)-one derivatives as potent CDK5 inhibitors.
Bioorganic & medicinal chemistry letters 2007;17(19):5384-9.
2007: Narender R Gavva; Anthony W Bannon; David N Hovland; Sonya G Lehto; Lana Klionsky; Sekhar Surapaneni; David C Immke; Charles Henley; Leyla Arik; Annette Bak; James Davis; Nadia Ernst; Gal Hever; Rongzhen Kuang; Licheng Shi; Rami Tamir; Jue Wang; Weiya Wang; Gary Zajic; Dawn Zhu; Mark H Norman; Jean-Claude Louis; Ella Magal; James J S Treanor
Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade.
The Journal of pharmacology and experimental therapeutics 2007;323(1):128-37.
2007: Hui-Ling Wang; Jodie Katon; Chenera Balan; Anthony W Bannon; Charles Bernard; Elizabeth M Doherty; Celia Dominguez; Narender R Gavva; Vijay K Gore; Vu V Ma; Nobuko Nishimura; Sekhar Surapaneni; Phi Tang; Rami Tamir; Oliver Thiel; James J S Treanor; Mark H Norman
Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties.
Journal of medicinal chemistry 2007;50(15):3528-39.
2007: Elizabeth M Doherty; Christopher Fotsch; Anthony W Bannon; Yunxin Bo; Ning Chen; Celia Dominguez; James Falsey; Narender R Gavva; Jodie Katon; Thomas Nixey; Vassil I Ognyanov; Liping Pettus; Robert M Rzasa; Markian Stec; Sekhar Surapaneni; Rami Tamir; Jiawang Zhu; James J S Treanor; Mark H Norman
Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate.
Journal of medicinal chemistry 2007;50(15):3515-27.
2007: Mark H Norman; Jiawang Zhu; Christopher Fotsch; Yunxin Bo; Ning Chen; Partha P Chakrabarti; Elizabeth M Doherty; Narender R Gavva; Nobuko Nishimura; Thomas Nixey; Vassil I Ognyanov; Robert M Rzasa; Markian Stec; Sekhar Surapaneni; Rami Tamir; Vellarkad Viswanadhan; James J S Treanor
Novel vanilloid receptor-1 antagonists: 1. Conformationally restricted analogues of trans-cinnamides.
Journal of medicinal chemistry 2007;50(15):3497-514.
2007: Alexandre A Steiner; Victoria F Turek; Maria C Almeida; Jeffrey J Burmeister; Daniela L Oliveira; Jennifer L Roberts; Anthony W Bannon; Mark H Norman; Jean-Claude Louis; James J S Treanor; Narender R Gavva; Andrej A Romanovsky
Nonthermal activation of transient receptor potential vanilloid-1 channels in abdominal viscera tonically inhibits autonomic cold-defense effectors.
The Journal of neuroscience : the official journal of the Society for Neuroscience 2007;27(28):7459-68.
2007: Narender R Gavva; Anthony W Bannon; Sekhar Surapaneni; David N Hovland; Sonya G Lehto; Anu Gore; Todd Juan; Hong Deng; Bora Han; Lana Klionsky; Rongzhen Kuang; April Le; Rami Tamir; Jue Wang; Brad Youngblood; Dawn Zhu; Mark H Norman; Ella Magal; James J S Treanor; Jean-Claude Louis
The vanilloid receptor TRPV1 is tonically activated in vivo and involved in body temperature regulation.
The Journal of neuroscience : the official journal of the Society for Neuroscience 2007;27(13):3366-74.
2007: Derin C D'Amico; Toshi Aya; Jason Human; Christopher Fotsch; Jian Jeffrey Chen; Kaustav Biswas; Bobby Riahi; Mark H Norman; Christopher A Willoughby; Randall W Hungate; Paul J Reider; Gloria Biddlecome; Dianna Lester-Zeiner; Carlo Van Staden; Eileen Johnson; Augustus Kamassah; Leyla Arik; Judy Wang; Vellarkad Viswanadhan; Robert D Groneberg; James Zhan; Hideo Suzuki; Andras Toro; David A Mareska; David E Clarke; Darren M Harvey; Laurence E Burgess; Ellen R Laird; Benny C Askew; Gordon Ng
Identification of a nonpeptidic and conformationally restricted bradykinin B1 receptor antagonist with anti-inflammatory activity.
Journal of medicinal chemistry 2007;50(4):607-10.
2006: Vassil I Ognyanov; Chenera Balan; Anthony W Bannon; Yunxin Bo; Celia Dominguez; Christopher Fotsch; Vijay K Gore; Lana Klionsky; Vu V Ma; Yi-Xin Qian; Rami Tamir; Xianghong Wang; Ning Xi; Shimin Xu; Dawn Zhu; Narender R Gavva; James J S Treanor; Mark H Norman
Design of potent, orally available antagonists of the transient receptor potential vanilloid 1. Structure-activity relationships of 2-piperazin-1-yl-1H-benzimidazoles.
Journal of medicinal chemistry 2006;49(12):3719-42.
2005: Ning Xi; Yunxin Bo; Elizabeth M Doherty; Christopher Fotsch; Narender R Gavva; Nianhe Han; Randall W Hungate; Lana Klionsky; Qingyian Liu; Rami Tamir; Shimin Xu; James J S Treanor; Mark H Norman
Synthesis and evaluation of thiazole carboxamides as vanilloid receptor 1 (TRPV1) antagonists.
Bioorganic & medicinal chemistry letters 2005;15(23):5211-7.
2005: Narender R Gavva; Rami Tamir; Lana Klionsky; Mark H Norman; Jean-Claude Louis; Kenneth D Wild; James J S Treanor
Proton activation does not alter antagonist interaction with the capsaicin-binding pocket of TRPV1.
Molecular pharmacology 2005;68(6):1524-33.
2005: Narender R Gavva; Rami Tamir; Yusheng Qu; Lana Klionsky; Tie J Zhang; David C Immke; Judy Wang; Dawn Zhu; Todd W Vanderah; Frank Porreca; Elizabeth M Doherty; Mark H Norman; Kenneth D Wild; Anthony W Bannon; Jean-Claude Louis; James J S Treanor
AMG 9810 [(E)-3-(4-t-butylphenyl)-N-(2,3-dihydrobenzo[b][1,4] dioxin-6-yl)acrylamide], a novel vanilloid receptor 1 (TRPV1) antagonist with antihyperalgesic properties.
The Journal of pharmacology and experimental therapeutics 2005;313(1):474-84.
2005: Christopher Fotsch; Nianhe Han; Premilla Arasasingham; Yunxin Bo; Michelle Carmouche; Ning Chen; James Davis; Martin H Goldberg; Clarence Hale; Feng-Yin Hsieh; Michael G Kelly; Qingyian Liu; Mark H Norman; Duncan M Smith; Markian Stec; Nuria A Tamayo; Ning Xi; Shimin Xu; Anthony W Bannon; James W Baumgartner
Melanocortin subtype-4 receptor agonists containing a piperazine core with substituted aryl sulfonamides.
Bioorganic & medicinal chemistry letters 2005;15(6):1623-7.
2005: Elizabeth M Doherty; Christopher Fotsch; Yunxin Bo; Partha P Chakrabarti; Ning Chen; Narender R Gavva; Nianhe Han; Michael G Kelly; John Kincaid; Lana Klionsky; Qingyian Liu; Vassil I Ognyanov; Rami Tamir; Xianghong Wang; Jiawang Zhu; Mark H Norman; James J S Treanor
Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides.
Journal of medicinal chemistry 2005;48(1):71-90.
2004: Ning Xi; Clarence Hale; Michael G Kelly; Mark H Norman; Markian Stec; Shimin Xu; James W Baumgartner; Christopher Fotsch
Synthesis of novel melanocortin 4 receptor agonists and antagonists containing a succinamide core.
Bioorganic & medicinal chemistry letters 2004;14(2):377-81.
2003: Christopher Fotsch; Duncan M Smith; Jeffrey A Adams; Janet Cheetham; Michael Croghan; Elizabeth M Doherty; Clarence Hale; Mark Jarosinski; Michael G Kelly; Mark H Norman; Nuria A Tamayo; Ning Xi; James W Baumgartner
Design of a new peptidomimetic agonist for the melanocortin receptors based on the solution structure of the peptide ligand, Ac-Nle-cyclo[Asp-Pro-DPhe-Arg-Trp-Lys]-NH(2).
Bioorganic & medicinal chemistry letters 2003;13(14):2337-40.
2003: Premilla N Arasasingham; Christopher Fotsch; Xiaohu Ouyang; Mark H Norman; Michael G Kelly; Kevin L Stark; Bill Karbon; Clarence Hale; James W Baumgartner; Martha Zambrano; Janet Cheetham; Nuria A Tamayo
Structure-activity relationship of (1-aryl-2-piperazinylethyl)piperazines: antagonists for the AGRP/melanocortin receptor binding.
Journal of medicinal chemistry 2003;46(1):9-11.
2001: Christopher Fotsch; J D Sonnenberg; Ning Chen; Clarence Hale; W Karbon; Mark H Norman
Synthesis and structure-activity relationships of trisubstituted phenyl urea derivatives as neuropeptide Y5 receptor antagonists.
Journal of medicinal chemistry 2001;44(14):2344-56.
2000: Mark H Norman; Ning Chen; Z Chen; Christopher Fotsch; Clarence Hale; Nianhe Han; R Hurt; T Jenkins; J Kincaid; L Liu; Y Lu; O Moreno; Vincent J Santora; J D Sonnenberg; W Karbon
Structure-activity relationships of a series of pyrrolo[3,2-d]pyrimidine derivatives and related compounds as neuropeptide Y5 receptor antagonists.
Journal of medicinal chemistry 2000;43(22):4288-312.
2000: Anthony W Bannon; J Seda; Michelle Carmouche; J M Francis; Mark H Norman; B Karbon; MICHAEL MCCALEB
Behavioral characterization of neuropeptide Y knockout mice.
Brain research 2000;868(1):79-87.
2000: N Chen; Y Lu; K Gadamasetti; C R Hurt; Mark H Norman; Christopher Fotsch
A short, facile synthesis of 5-substituted 3-amino-1H-pyrrole-2-carboxylates.
The Journal of organic chemistry 2000;65(8):2603-5.