R. Bhide

发表

The Antiangiogenic Activity in Xenograft Models of Brivanib, a Dual Inhibitor of Vascular Endothelial Growth Factor Receptor-2 and Fibroblast Growth Factor Receptor-1 Kinases

J. Fargnoli, J. Barrish, J. Hunt, 2010, Molecular Cancer Therapeutics.

RATIONAL DESIGN OF POTENT CARBOXYLIC ACID BASED BISUBSTRATE INHIBITORS OF RAS FARNESYL PROTEIN TRANSFERASE

S. Robinson, D. Patel, L. Hunihan, 1994 .

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.

J. Fargnoli, J. Barrish, J. Tokarski, 2005, Journal of medicinal chemistry.

Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor.

Punit Marathe, Ravindra Tejwani, Arvind Mathur, 2008, Bioorganic & medicinal chemistry letters.

Metabolism of 5-Isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737): Identification of an Unusual N-Acetylglucosamine Conjugate in the Cynomolgus Monkey

Y. Shu, Donna D Wei, L. Qian, 2008, Drug Metabolism and Disposition.

Concise and efficient synthesis of 4-fluoro-1H-pyrrolo[2,3-b]pyridine.

R. Ruel, R. Bhide, A. L’Heureux, 2003, Organic letters.

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)

J. Fargnoli, G. Derbin, J. Barrish, 2008, Journal of medicinal chemistry.

Design, synthesis, and structure-activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors.

J. Tokarski, B. Koplowitz, J. Hunt, 2005, Bioorganic & medicinal chemistry letters.

Synthesis and SAR of pyrrolotriazine-4-one based Eg5 inhibitors.

L. Mueller, S. Sheriff, David K. Williams, 2006, Bioorganic & medicinal chemistry letters.

Optimization of Nicotinamides as Potent and Selective IRAK4 Inhibitors with Efficacy in a Murine Model of Psoriasis.

J. Barrish, D. Xie, N. Murugesan, 2020, ACS medicinal chemistry letters.

Discovery and SAR of pyrrolo[2,1-f][1,2,4]triazin-4-amines as potent and selective PI3Kδ inhibitors.

C. Weigelt, M. Poss, J. Sack, 2016, Bioorganic & medicinal chemistry letters.

Identification of highly potent and selective PI3Kδ inhibitors.

G. Schieven, C. Weigelt, M. Poss, 2017, Bioorganic & medicinal chemistry letters.

Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders.

K. McIntyre, Sidney Pitt, G. Schieven, 2017, Journal of medicinal chemistry.

Discovery of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent and selective PI3Kδ inhibitors.

C. Weigelt, M. Poss, J. Sack, 2017, Bioorganic & medicinal chemistry letters.

Development of highly potent inhibitors of Ras farnesyltransferase possessing cellular and in vivo activity.

M. Barbacid, B. Seizinger, J. Hunt, 1996, Journal of medicinal chemistry.

Discovery of the pyrrolo[2,1-f][1,2,4]triazine nucleus as a new kinase inhibitor template.

J. Fargnoli, J. Hunt, B. Fink, 2004, Journal of medicinal chemistry.

A chiral bicyclic intermediate for the synthesis of forskolin

G. Bold, Shih-Hsiung Wu, D. Patel, 1987 .

Di-tert-butylmethylsilyl (DTBMS) trifluoromethanesulfonate. Preparation and synthetic applications of DTBMS esters and enol ethers

B. Levison, R. G. Salomon, R. Bhide, 1986 .

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.

J. Fargnoli, G. Derbin, J. Barrish, 2006, Journal of medicinal chemistry.

Synthesis and SAR of 4-(3-hydroxyphenylamino)pyrrolo[2,1-f][1,2,4]triazine based VEGFR-2 kinase inhibitors.

J. Fargnoli, J. Tokarski, J. Hunt, 2005, Bioorganic & medicinal chemistry letters.

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.

S. Chong, J. Hunt, Soong-Hoon Kim, 2000, Journal of medicinal chemistry.

Preclinical pharmacokinetics and in vitro metabolism of brivanib (BMS-540215), a potent VEGFR2 inhibitor and its alanine ester prodrug brivanib alaninate

J. Fargnoli, A. Kamath, P. Marathe, 2009, Cancer Chemotherapy and Pharmacology.

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.

J. Fargnoli, G. Derbin, J. Barrish, 2006, Journal of medicinal chemistry.

Discovery and structure-activity relationships of imidazole-containing tetrahydrobenzodiazepine inhibitors of farnesyltransferase.

J. Hunt, V. Manne, C. Ricca, 1999, Journal of medicinal chemistry.

Discovery of Brivanib Alaninate: A Dual Vascular Endothelial Growth Factor and Fibroblast Growth Factor Receptor Inhibitor

J. Fargnoli, R. Bhide, 2009 .

Discovery and structure-based design of 4,6-diaminonicotinamides as potent and selective IRAK4 inhibitors.

S. Spergel, C. Weigelt, M. Poss, 2017, Bioorganic & medicinal chemistry letters.

J. Fargnoli, G. Derbin, J. Barrish, 2008, Bioorganic & medicinal chemistry letters.

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.

J. Fargnoli, J. Tokarski, J. Hunt, 2008, Bioorganic & medicinal chemistry letters.

Y. Shu, L. Qian, A. Kamath, 2008, Drug Metabolism and Disposition.

Dasatinib (BMS-354825) Overcomes Multiple Mechanisms of Imatinib Resistance in Chronic Myeloid Leukemia (CML).

F. Lee, R. Borzilleri, L. Lombardo, 2005 .

Synthesis and SAR of 4‐(3‐Hydroxyphenylamino)pyrrolo[2,1‐f][1,2,4]triazine Based VEGFR‐2 Kinase Inhibitors.

R. Bhide, 2005 .

Discovery of BMS-986308: A Renal Outer Medullary Potassium Channel Inhibitor for the Treatment of Heart Failure.

A. Mathur, E. Priestley, J. M. Richter, 2024, Journal of medicinal chemistry.