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Your search keyword '"Weifang Shan"' showing total 2 results
Start Over Author "Weifang Shan" Journal acs medicinal chemistry letters
2 results on '"Weifang Shan"'

1. Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer

Author

Janet Dell-John, John D. Dimarco, Cheryl A. Rizzo, Mark E. Salvati, Steven H. Spergel, Gregory Scott Martin, Weifang Shan, Aaron Balog, Georgia Cornelius, Richard Rampulla, Marco M. Gottardis, Andrew Nation, Christian L. Holst, Liang Schweizer, Gregory D. Vite, Lana M. Rossiter, Ricardo M. Attar, David J. Fairfax, Thomas E. Spires, Stanley R. Krystek, George L. Trainor, and Jack Z. Gougoutas

Subjects
Nonsteroidal, Bicalutamide, business.industry, digestive, oral, and skin physiology, Organic Chemistry, Antagonist, Cancer, Pharmacology, medicine.disease, Biochemistry, In vitro, Androgen receptor, stomatognathic diseases, Prostate cancer, chemistry.chemical_compound, chemistry, Drug Discovery, Medicine, Androgen receptor antagonist, business, medicine.drug
Abstract

BMS-641988 (23) is a novel, nonsteroidal androgen receptor antagonist designed for the treatment of prostate cancer. The compound has high binding affinity for the AR and acts as a functional antagonist in vitro. BMS-641988 is efficacious in multiple human prostate cancer xenograft models, including CWR22-BMSLD1 where it displays superior efficacy relative to bicalutamide. Based on its promising preclinical profile, BMS-641988 was selected for clinical development.

Published
2015
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2. Discovery of Clinical Candidate BMS-906024: A Potent Pan-Notch Inhibitor for the Treatment of Leukemia and Solid Tumors

Author

Claude A. Quesnelle, Patrice Gill, Richard Rampulla, Ching Su, Gerry Everlof, George L. Trainor, Ke Chen, Vinod Arora, Richard A. Westhouse, Celia D’Arienzo, Andrew J. Tebben, Weifang Shan, John T. Hunt, Derek J. Norris, Louis J. Lombardo, Zheng Yang, Arvind Mathur, Mei-Li Wen, Yingru Zhang, Dauh-Rurng Wu, Wen-Ching Han, Krista Menard, Victor R. Guarino, Asoka Ranasinghe, Richard E. Olson, Ashvinikumar V. Gavai, Bruce S. Fischer, Phil S. Baran, Anne Rose, Lan Xiao, Ronald E. White, Mary Ellen Cvijic, Gregory D. Vite, Ding Ren Shen, Jere E. Meredith, Haiqing Wang, Francis Y. Lee, and Aaron Balog

Subjects
business.industry, Organic Chemistry, Pharmacology, medicine.disease, Biochemistry, T Acute Lymphoblastic Leukemia, Leukemia, In vivo, Drug Discovery, medicine, Receptor, business, Solid tumor, Clinical evaluation, Triple-negative breast cancer
Abstract

Structure-activity relationships in a series of (2-oxo-1,4-benzodiazepin-3-yl)-succinamides identified highly potent inhibitors of γ-secretase mediated signaling of Notch1/2/3/4 receptors. On the basis of its robust in vivo efficacy at tolerated doses in Notch driven leukemia and solid tumor xenograft models, 12 (BMS-906024) was selected as a candidate for clinical evaluation.

Published
2015
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