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John Hunt

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Zhen-Wei Cai; Donna Wei; Gretchen M Schroeder; Lyndon A M Cornelius; Kyoung Kim; Xiao-Tao Chen; Robert J Schmidt; David K Williams; John S Tokarski; Yongmi An; John S Sack; swam manne; Amrita V Kamath; Yueping Zhang; Punit Marathe; John T Hunt; Louis J Lombardo; Joseph Fargnoli; Robert M Borzilleri
Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors.
Zhen-Wei Cai; Yongzheng Zhang; Robert M Borzilleri; Ligang Qian; Stephanie Barbosa; Donna Wei; Xiaoping Zheng; Lawrence Wu; Junying Fan; Zhongping Shi; Barri Wautlet; Steven Mortillo; Robert Jeyaseelan; Daniel W Kukral; Amrita V Kamath; Punit Marathe; Celia D'Arienzo; George Derbin; Joel C Barrish; Jeffrey A Robl; John T Hunt; Louis J Lombardo; Joseph Fargnoli; Rajeev S Bhide
Discovery of brivanib alaninate ((S)-((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl)2-aminopropanoate), a novel prodrug of dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 kinase inhibitor (BMS-540215).
Gretchen M Schroeder; Xiao-Tao Chen; David K Williams; David S Nirschl; Zhen-Wei Cai; Donna Wei; John S Tokarski; Yongmi An; John Sack; Zhong Chen; Tram Huynh; Wayne Vaccaro; Michael Poss; Barri Wautlet; Johnni Gullo-Brown; Kristen A Kellar; swam manne; John T Hunt; Tze Wai Wong; Louis J Lombardo; Joseph Fargnoli; Robert M Borzilleri
Identification of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Met kinase.

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All Publications

2008: Zhen-Wei Cai; Donna Wei; Gretchen M Schroeder; Lyndon A M Cornelius; Kyoung Kim; Xiao-Tao Chen; Robert J Schmidt; David K Williams; John S Tokarski; Yongmi An; John S Sack; swam manne; Amrita V Kamath; Yueping Zhang; Punit Marathe; John T Hunt; Louis J Lombardo; Joseph Fargnoli; Robert M Borzilleri
Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors.
Bioorganic & medicinal chemistry letters 2008;18(11):3224-9.
2008: Zhen-Wei Cai; Yongzheng Zhang; Robert M Borzilleri; Ligang Qian; Stephanie Barbosa; Donna Wei; Xiaoping Zheng; Lawrence Wu; Junying Fan; Zhongping Shi; Barri Wautlet; Steven Mortillo; Robert Jeyaseelan; Daniel W Kukral; Amrita V Kamath; Punit Marathe; Celia D'Arienzo; George Derbin; Joel C Barrish; Jeffrey A Robl; John T Hunt; Louis J Lombardo; Joseph Fargnoli; Rajeev S Bhide
Discovery of brivanib alaninate ((S)-((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl)2-aminopropanoate), a novel prodrug of dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 kinase inhibitor (BMS-540215).
Journal of medicinal chemistry 2008;51(6):1976-80.
2008: Gretchen M Schroeder; Xiao-Tao Chen; David K Williams; David S Nirschl; Zhen-Wei Cai; Donna Wei; John S Tokarski; Yongmi An; John Sack; Zhong Chen; Tram Huynh; Wayne Vaccaro; Michael Poss; Barri Wautlet; Johnni Gullo-Brown; Kristen A Kellar; swam manne; John T Hunt; Tze Wai Wong; Louis J Lombardo; Joseph Fargnoli; Robert M Borzilleri
Identification of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Met kinase.
Bioorganic & medicinal chemistry letters 2008;18(6):1945-51.
2008: Zhen-Wei Cai; Donna Wei; Robert M Borzilleri; Ligang Qian; Amrita V Kamath; Steven Mortillo; Barri Wautlet; Benjamin J Henley; Robert Jeyaseelan; John S Tokarski; John T Hunt; Rajeev S Bhide; Joseph Fargnoli; Louis J Lombardo
Synthesis, SAR, and Evaluation of 4-[2,4-Difluoro-5-(cyclopropylcarbamoyl)phenylamino]pyrrolo[2,1-f][1,2,4]triazine-based VEGFR-2 kinase inhibitors.
Bioorganic & medicinal chemistry letters 2008;18(4):1354-8.
2006: Tze Wai Wong; Francis Y Lee; Chiang Yu; Feng R Luo; Simone Oppenheimer; Hongjian Zhang; Richard A Smykla; Harold Mastalerz; Brian E Fink; John T Hunt; Ashvinikumar V Gavai; Gregory D Vite
Preclinical antitumor activity of BMS-599626, a pan-HER kinase inhibitor that inhibits HER1/HER2 homodimer and heterodimer signaling.
Clinical cancer research : an official journal of the American Association for Cancer Research 2006;12(20 Pt 1):6186-93.
2006: Robert M Borzilleri; Rajeev S Bhide; Joel C Barrish; Celia J D'Arienzo; George M Derbin; Joseph Fargnoli; John T Hunt; Robert Jeyaseelan; Amrita V Kamath; Daniel W Kukral; Punit Marathe; Steven Mortillo; Ligang Qian; John S Tokarski; Barri Wautlet; Xiaoping Zheng; Louis J Lombardo
Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.
Journal of medicinal chemistry 2006;49(13):3766-9.
2006: Rajeev S Bhide; Zhen-Wei Cai; Yong-Zheng Zhang; Ligang Qian; Donna Wei; Stephanie A Barbosa; Louis J Lombardo; Robert M Borzilleri; Xiaoping Zheng; Laurence I Wu; Joel C Barrish; Soong-Hoon Kim; Kenneth J Leavitt; Arvind Mathur; Leslie Leith; Sam Chao; Barri Wautlet; Steven Mortillo; Robert Jeyaseelan; Daniel W Kukral; John T Hunt; Amrita V Kamath; Aberra Fura; Viral Vyas; Punit Marathe; Celia D'Arienzo; George Derbin; Joseph Fargnoli
Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.
Journal of medicinal chemistry 2006;49(7):2143-6.
2005: Brian E Fink; Gregory D Vite; Harold Mastalerz; John F Kadow; Soong-Hoon Kim; Kenneth J Leavitt; Karen Du; Donald Crews; Toomas Mitt; Tze Wai Wong; John T Hunt; Dolatrai M Vyas; John S Tokarski
New dual inhibitors of EGFR and HER2 protein tyrosine kinases.
Bioorganic & medicinal chemistry letters 2005;15(21):4774-9.
2005: Robert M Borzilleri; Xiaoping Zheng; Ligang Qian; Christopher D Ellis; Zhen-Wei Cai; Barri Wautlet; Steven Mortillo; Robert Jeyaseelan; Daniel W Kukral; Aberra Fura; Amrita V Kamath; Viral Vyas; John S Tokarski; Joel C Barrish; John T Hunt; Louis J Lombardo; Joseph Fargnoli; Rajeev S Bhide
Design, synthesis, and evaluation of orally active 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors.
Journal of medicinal chemistry 2005;48(12):3991-4008.
2005: Louis J Lombardo; Amy Camuso; John Clark; Krista Fager; Johnni Gullo-Brown; John T Hunt; Ivan Inigo; David Kan; Barry Koplowitz; Francis Lee; Kelly McGlinchey; Ligang Qian; Carolyn S Ricca; George Rovnyak; Sarah C Traeger; John S Tokarski; David K Williams; Laurence I Wu; Yufen Zhao; swam manne; Rajeev S Bhide
Design, synthesis, and structure-activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors.
Bioorganic & medicinal chemistry letters 2005;15(7):1895-9.
2005: Robert M Borzilleri; Zhen-Wei Cai; Christopher D Ellis; Joseph Fargnoli; Aberra Fura; Tracy Gerhardt; Bindu Goyal; John T Hunt; Steven Mortillo; Ligang Qian; John S Tokarski; Viral Vyas; Barri Wautlet; Xioping Zheng; Rajeev S Bhide
Synthesis and SAR of 4-(3-hydroxyphenylamino)pyrrolo[2,1-f][1,2,4]triazine based VEGFR-2 kinase inhibitors.
Bioorganic & medicinal chemistry letters 2005;15(5):1429-33.
2005: Mark E Salvati; Aaron Balog; Donna D Wei; Dacia Pickering; Ricardo M Attar; Jieping Geng; Cheryl A Rizzo; John T Hunt; Marco Gottardis; roberto weinmann; Rogelio Martinez
Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus.
Bioorganic & medicinal chemistry letters 2005;15(2):389-93.
2004: Louis J Lombardo; Francis Y Lee; Ping Chen; Derek Norris; Joel C Barrish; Kamelia Behnia; Stephen Castaneda; Lyndon A Cornelius; Jagabandhu Das; Arthur M Doweyko; Craig R Fairchild; John T Hunt; Ivan Inigo; Kathy Johnston; Amrita V Kamath; David Kan; Herbert E Klei; Punit Marathe; Suhong Pang; Russell Peterson; Sidney Pitt; Gary L Schieven; Robert J Schmidt; John S Tokarski; Mei-Li Wen; John Wityak; Robert M Borzilleri
Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.
Journal of medicinal chemistry 2004;47(27):6658-61.
2004: Aaron Balog; Mark E Salvati; Weifang Shan; Arvind Mathur; Leslie Leith; Donna D Wei; Ricardo M Attar; Jieping Geng; Cheryl A Rizzo; Chihuei Wang; Stanley R Krystek; John S Tokarski; John T Hunt; Marco Gottardis; roberto weinmann
The synthesis and evaluation of [2.2.1]-bicycloazahydantoins as androgen receptor antagonists.
Bioorganic & medicinal chemistry letters 2004;14(24):6107-11.
2004: John T Hunt; Toomas Mitt; Robert M Borzilleri; Johnni Gullo-Brown; Joseph Fargnoli; Brian Fink; Wen-Ching Han; Steven Mortillo; Gregory D Vite; Barri Wautlet; Tai Wong; Chiang Yu; Xiaoping Zheng; Rajeev S Bhide
Discovery of the pyrrolo[2,1-f][1,2,4]triazine nucleus as a new kinase inhibitor template.
Journal of medicinal chemistry 2004;47(16):4054-9.
2004: swam manne; Francis Y Lee; David K Bol; Johnni Gullo-Brown; Craig R Fairchild; Louis J Lombardo; Richard A Smykla; Gregory D Vite; Mei-Li Wen; Chiang Yu; Tze Wai Wong; John T Hunt
Apoptotic and cytostatic farnesyltransferase inhibitors have distinct pharmacology and efficacy profiles in tumor models.
Cancer research 2004;64(11):3974-80.
2004: Raj Misra; Hai-yun Xiao; Kyoung S Kim; Songfeng Lu; Wen-Ching Han; Stephanie A Barbosa; John T Hunt; David B Rawlins; Weifang Shan; Syed Z Ahmed; Ligang Qian; Bang-Chi Chen; Rulin Zhao; Mark S Bednarz; Kristen A Kellar; Janet G Mulheron; Roberta Batorsky; Urvashi Roongta; Amrita V Kamath; Punit Marathe; Sunanda A Ranadive; John S Sack; John S Tokarski; Nikola P Pavletich; Francis Y Lee; Kevin R Webster; S David Kimball
N-(cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4- piperidinecarboxamide (BMS-387032), a highly efficacious and selective antitumor agent.
Journal of medicinal chemistry 2004;47(7):1719-28.
2002: Kyoung Soon Kim; S David Kimball; Raj Misra; David B Rawlins; John T Hunt; Hai-yun Xiao; Songfeng Lu; Ligang Qian; Wen-Ching Han; Weifang Shan; Toomas Mitt; Zhen-Wei Cai; Michael A Poss; Hong Zhu; John S Sack; John S Tokarski; Chieh Ying Chang; Nikola P Pavletich; Amrita V Kamath; W Griffith Humphreys; Punit Marathe; Isia Bursuker; Kristen A Kellar; Urvashi Roongta; Roberta Batorsky; Janet G Mulheron; David K Bol; Craig R Fairchild; Francis Y Lee; Kevin R Webster
Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities.
Journal of medicinal chemistry 2002;45(18):3905-27.
2000: Kyoung Soon Kim; John S Sack; John S Tokarski; Ligang Qian; S T Chao; Leslie Leith; YF Kelly; Raj Misra; John T Hunt; S David Kimball; W Griffith Humphreys; Barri Wautlet; Janet G Mulheron; Kevin R Webster
Thio- and oxoflavopiridols, cyclin-dependent kinase 1-selective inhibitors: synthesis and biological effects.
Journal of medicinal chemistry 2000;43(22):4126-34.
2000: John T Hunt; CZ Ding; Roberta Batorsky; Mark S Bednarz; Rajeev S Bhide; Y Cho; S Chong; Sam Chao; Johnni Gullo-Brown; P Guo; Soong-Hoon Kim; Francis Y Lee; Katerina Leftheris; A Miller; Toomas Mitt; M Patel; B A Penhallow; Carolyn S Ricca; William C Rose; R Schmidt; William A Slusarchyk; Gregory D Vite; swam manne
Discovery of (R)-7-cyano-2,3,4, 5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3- (phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine (BMS-214662), a farnesyltransferase inhibitor with potent preclinical antitumor activity.
Journal of medicinal chemistry 2000;43(20):3587-95.
2000: CZ Ding; John T Hunt; Carolyn S Ricca; swam manne
3-Imidazolylmethylaminophenylsulfonyltetrahydroquinolines, a novel series of farnesyltransferase inhibitors.
Bioorganic & medicinal chemistry letters 2000;10(3):273-5.
1999: CZ Ding; Roberta Batorsky; Rajeev S Bhide; H J Chao; Y Cho; S Chong; Johnni Gullo-Brown; P Guo; Soong-Hoon Kim; Francis Lee; Katerina Leftheris; A Miller; Toomas Mitt; M Patel; B A Penhallow; Carolyn S Ricca; William C Rose; R Schmidt; William A Slusarchyk; Gregory D Vite; N Yan; swam manne; John T Hunt
Discovery and structure-activity relationships of imidazole-containing tetrahydrobenzodiazepine inhibitors of farnesyltransferase.
Journal of medicinal chemistry 1999;42(25):5241-53.
1998: Natesan Murugesan; Zhengxiang Gu; Philip D Stein; Sharon N Bisaha; Steven H Spergel; RN Girotra; V G Lee; John Lloyd; Raj Misra; J Schmidt; Arvind Mathur; L Stratton; YF Kelly; Eileen Bird; Tom Waldron; Eddie C-K Liu; Rongan Zhang; H Lee; RP Serafino; Benoni E Abboa-Offei; P Mathers; Mary Giancarli; AA Seymour; Maria L Webb; John T Hunt
Biphenylsulfonamide endothelin antagonists: structure-activity relationships of a series of mono- and disubstituted analogues and pharmacology of the orally active endothelin antagonist 2'-amino-N- (3,4-dimethyl-5-isoxazolyl)-4'-(2-methylpropyl)[1, 1'-biphenyl]-2-sulfonamide (BMS-187308).
Journal of medicinal chemistry 1998;41(26):5198-218.
1996: John T Hunt; V G Lee; K Leftheris; B Seizinger; J Carboni; J Mabus; C Ricca; N Yan; swam manne
Potent, cell active, non-thiol tetrapeptide inhibitors of farnesyltransferase.
Journal of medicinal chemistry 1996;39(2):353-8.
1996: K Leftheris; T Kline; G D Vite; Y H Cho; R S Bhide; D V Patel; M M Patel; R J Schmidt; H N Weller; M L Andahazy; J M Carboni; J L Gullo-Brown; F Y Lee; C Ricca; W C Rose; N Yan; Mariano Barbacid; John T Hunt; C A Meyers; B R Seizinger; Robert Zahler; swam manne
Development of highly potent inhibitors of Ras farnesyltransferase possessing cellular and in vivo activity.
Journal of medicinal chemistry 1996;39(1):224-36.
1995: S Natarajan; John T Hunt; S Festin; R Serafino; R Zhang; S Moreland
Endothelin analogs which distinguish vasoconstrictor and vasodilator ETB receptors.
Life sciences 1995;56(15):1251-6.
1995: S R Krystek; John T Hunt; P D Stein; T R Stouch
Three-dimensional quantitative structure-activity relationships of sulfonamide endothelin inhibitors.
Journal of medicinal chemistry 1995;38(4):659-68.
1995: Niels H Andersen; S M Harris; V G Lee; E C Liu; S Moreland; John T Hunt
The receptor binding affinity of monocyclic [Ala3,Xaa11]endothelin-1 analogs correlates with inducible helix length.
Bioorganic & medicinal chemistry 1995;3(2):113-24.
1994: P D Stein; John T Hunt; D M Floyd; S Moreland; Kenneth Dickinson; C Mitchell; E C Liu; Maria L Webb; N Murugesan; J Dickey
The discovery of sulfonamide endothelin antagonists and the development of the orally active ETA antagonist 5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulf onamide.
Journal of medicinal chemistry 1994;37(3):329-31.
1993: S D Kimball; John T Hunt; J C Barrish; J Das; D M Floyd; M W Lago; V G Lee; S H Spergel; S Moreland; S A Hedberg
1-Benzazepin-2-one calcium channel blockers--VI. Receptor-binding model and possible relationship to desmethoxyverapamil.
Bioorganic & medicinal chemistry 1993;1(4):285-307.
1993: John T Hunt; V G Lee; E C Liu; S Moreland; D McMullen; Maria L Webb; M Bolgar
Control of peptide disulfide regioisomer formation by mixed cysteine-penicillamine bridges. Application to endothelin-1.
International journal of peptide and protein research 1993;42(3):249-58.
1993: John T Hunt; V G Lee; D McMullen; E C Liu; M Bolgar; C L Delaney; S M Festin; D M Floyd; A Hedberg; S Natarajan
Structure-activity studies of endothelin leading to novel peptide ETA antagonists.
Bioorganic & medicinal chemistry 1993;1(1):59-65.
1992: S Natarajan; S M Festin; A Hedberg; E C Liu; D M Floyd; John T Hunt
Site-specific biotinylation. A novel approach and its application to endothelin-1 analogs and PTH-analog.
International journal of peptide and protein research 1992;40(6):567-74.
1992: S Moreland; M Ikebe; John T Hunt; Robert S Moreland
Peptide analogs of the pseudosubstrate domain of smooth muscle myosin light chain kinase inhibit actomyosin ATPase activity at concentrations that do not inhibit superprecipitation.
Biochemical and biophysical research communications 1992;187(3):1279-84.
1992: S Moreland; M Ikebe; John T Hunt; Robert S Moreland
Substrate based inhibitors of smooth muscle myosin light chain kinase.
Biochemical and biophysical research communications 1992;185(1):379-85.
1992: S Moreland; D M McMullen; C L Delaney; V G Lee; John T Hunt
Venous smooth muscle contains vasoconstrictor ETB-like receptors.
Biochemical and biophysical research communications 1992;184(1):100-6.
1992: S R Krystek; D A Bassolino; R E Bruccoleri; John T Hunt; M A Porubcan; C F Wandler; Niels H Andersen
Solution conformation of a cyclic pentapeptide endothelin antagonist. Comparison of structures obtained from constrained dynamics and conformational search.
FEBS letters 1992;299(3):255-61.
1992: S D Kimball; D M Floyd; J Das; John T Hunt; J Krapcho; George Rovnyak; K J Duff; V G Lee; R V Moquin; C F Turk
Benzazepinone calcium channel blockers. 4. Structure-activity overview and intracellular binding site.
Journal of medicinal chemistry 1992;35(4):780-93.
1991: Richard B Pearson; John T Hunt; Kenneth I Mitchelhill; B E Kemp
Myosin light chain kinase autoregulatory pseudosubstrate prototope.
Peptide research 1991;4(3):147-53, 156-7.
1991: AA Seymour; J A Norman; MM Asaad; S A Fennell; B Abboa-Offei; D K Little; V J Kratunis; N G Delaney; John T Hunt; G Di Donato
Possible regulation of atrial natriuretic factor by neutral endopeptidase 24.11 and clearance receptors.
The Journal of pharmacology and experimental therapeutics 1991;256(3):1002-9.
1989: John T Hunt; D M Floyd; V G Lee; D K Little; S Moreland
Minimum requirements for inhibition of smooth-muscle myosin light-chain kinase by synthetic peptides.
The Biochemical journal 1989;257(1):73-8.
1988: Richard B Pearson; D M Floyd; John T Hunt; V G Lee; B E Kemp
Hydroxyamino acid specificity of smooth muscle myosin light chain kinase.
Archives of biochemistry and biophysics 1988;260(1):37-44.