Literature DB >> 26288692

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

Aaron Balog1, Richard Rampulla1, Gregory S Martin2, Stanley R Krystek1, Ricardo Attar1, Janet Dell-John1, John D DiMarco1, David Fairfax2, Jack Gougoutas1, Christian L Holst2, Andrew Nation1, Cheryl Rizzo1, Lana M Rossiter2, Liang Schweizer1, Weifang Shan1, Steven Spergel1, Thomas Spires1, Georgia Cornelius1, Marco Gottardis1, George Trainor1, Gregory D Vite1, Mark E Salvati1.   

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.

Entities:  

Keywords:  BMS-641988; CRPC; Prostate cancer; androgen receptor

Year:  2015        PMID： 26288692      PMCID： PMC4538445          DOI： 10.1021/acsmedchemlett.5b00173

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  13 in total

1.  Myotrophic activity of 19-nortestosterone and other steroids determined by modified levator ani muscle method.

Authors:  L G HERSHBERGER; E G SHIPLEY; R K MEYER
Journal:  Proc Soc Exp Biol Med       Date:  1953-05

2.  Crystallographic structures of the ligand-binding domains of the androgen receptor and its T877A mutant complexed with the natural agonist dihydrotestosterone.

Authors:  J S Sack; K F Kish; C Wang; R M Attar; S E Kiefer; Y An; G Y Wu; J E Scheffler; M E Salvati; S R Krystek; R Weinmann; H M Einspahr
Journal:  Proc Natl Acad Sci U S A       Date:  2001-04-24       Impact factor: 11.205

3.  Flexible protein-ligand docking by global energy optimization in internal coordinates.

Authors:  M Totrov; R Abagyan
Journal:  Proteins       Date:  1997

Review 4.  Biology of progressive, castration-resistant prostate cancer: directed therapies targeting the androgen-receptor signaling axis.

Authors:  Howard I Scher; Charles L Sawyers
Journal:  J Clin Oncol       Date:  2005-11-10       Impact factor: 44.544

5.  Phase I dose-escalation study of the novel antiandrogen BMS-641988 in patients with castration-resistant prostate cancer.

Authors:  Dana Rathkopf; Glenn Liu; Michael A Carducci; Mario A Eisenberger; Aseem Anand; Michael J Morris; Susan F Slovin; Yasutsuna Sasaki; Shunji Takahashi; Seiichiro Ozono; Nga Kit Eliza Fung; Shinta Cheng; Jinping Gan; Marco Gottardis; Mary T Obermeier; Jyotsna Reddy; Steven Zhang; Blisse J Vakkalagadda; Leila Alland; George Wilding; Howard I Scher
Journal:  Clin Cancer Res       Date:  2010-12-03       Impact factor: 12.531

6.  Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus.

Authors:  Mark E Salvati; Aaron Balog; Donna D Wei; Dacia Pickering; Ricardo M Attar; Jieping Geng; Cheryl A Rizzo; John T Hunt; Marco M Gottardis; Roberto Weinmann; Rogelio Martinez
Journal:  Bioorg Med Chem Lett       Date:  2005-01-17       Impact factor: 2.823

7.  Androgen levels increase by intratumoral de novo steroidogenesis during progression of castration-resistant prostate cancer.

Authors:  Jennifer A Locke; Emma S Guns; Amy A Lubik; Hans H Adomat; Stephen C Hendy; Catherine A Wood; Susan L Ettinger; Martin E Gleave; Colleen C Nelson
Journal:  Cancer Res       Date:  2008-08-01       Impact factor: 12.701

8.  Identification and optimization of a novel series of [2.2.1]-oxabicyclo imide-based androgen receptor antagonists.

Authors:  Mark E Salvati; Aaron Balog; Weifang Shan; Richard Rampulla; Soren Giese; Tom Mitt; Joseph A Furch; Gregory D Vite; Ricardo M Attar; Maria Jure-Kunkel; Jieping Geng; Cheryl A Rizzo; Marco M Gottardis; Stanley R Krystek; Jack Gougoutas; Michael A Galella; Mary Obermeier; Aberra Fura; Gamini Chandrasena
Journal:  Bioorg Med Chem Lett       Date:  2008-02-08       Impact factor: 2.823

Review 9.  Current status of combined androgen blockade: optimal therapy for advanced prostate cancer.

Authors:  E D Crawford; E P DeAntoni
Journal:  J Clin Endocrinol Metab       Date:  1995-04       Impact factor: 5.958

10.  Enzalutamide for treatment of patients with metastatic castration-resistant prostate cancer who have previously received docetaxel: U.S. Food and Drug Administration drug approval summary.

Authors:  Yangmin M Ning; William Pierce; V Ellen Maher; Stella Karuri; Sheng-Hui Tang; Haw-Jyh Chiu; Todd Palmby; Jeanne Fourie Zirkelbach; Dhananjay Marathe; Nitin Mehrotra; Qi Liu; Debasis Ghosh; Christy L Cottrell; John Leighton; Rajeshwari Sridhara; Amna Ibrahim; Robert Justice; Richard Pazdur
Journal:  Clin Cancer Res       Date:  2013-10-18       Impact factor: 12.531
View more
  5 in total

Review 1.  Current advances in intratumoral androgen metabolism in castration-resistant prostate cancer.

Authors:  Trevor M Penning; Daniel Tamae
Journal:  Curr Opin Endocrinol Diabetes Obes       Date:  2016-06       Impact factor: 3.243

Review 2.  The Curtius Rearrangement: Applications in Modern Drug Discovery and Medicinal Chemistry.

Authors:  Arun K Ghosh; Margherita Brindisi; Anindya Sarkar
Journal:  ChemMedChem       Date:  2018-10-11       Impact factor: 3.466

3.  Paradoxical androgen receptor regulation by small molecule enantiomers.

Authors:  Katherin Patsch; Chao Liu; Grzegorz Zapotoczny; Yuanye Sun; Harish Sura; Nolan Ung; Ren X Sun; Bethany Haliday; Chen Yu; Mayada Aljehani; Jerry S H Lee; Boris A Kashemirov; David B Agus; Charles E McKenna; Daniel Ruderman
Journal:  Proc Natl Acad Sci U S A       Date:  2021-03-23       Impact factor: 12.779

Review 4.  Second generation androgen receptor antagonists and challenges in prostate cancer treatment.

Authors:  Yanhua Chen; Qianqian Zhou; William Hankey; Xiaosheng Fang; Fuwen Yuan
Journal:  Cell Death Dis       Date:  2022-07-21       Impact factor: 9.685

5.  Small Molecule Antagonists of the Nuclear Androgen Receptor for the Treatment of Castration-Resistant Prostate Cancer.

Authors:  James K Johnson; Erin M Skoda; Jianhua Zhou; Erica Parrinello; Dan Wang; Katherine O'Malley; Benjamin R Eyer; Mustafa Kazancioglu; Kurtis Eisermann; Paul A Johnston; Joel B Nelson; Zhou Wang; Peter Wipf
Journal:  ACS Med Chem Lett       Date:  2016-05-27       Impact factor: 4.345
  5 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.