2. Academic Validation
  3. A potent and highly efficacious Bcl-2/Bcl-xL inhibitor

A potent and highly efficacious Bcl-2/Bcl-xL inhibitor

  • J Med Chem. 2013 Apr 11;56(7):3048-3067. doi: 10.1021/jm4001105.
Angelo Aguilar  # 1,  Haibin Zhou  # 1,  Jianfang Chen  # 1,  Liu Liu  # 1,  Longchuan Bai  # 1,  Donna McEachern 1,  Chao-Yie Yang 1,  Jennifer Meagher 2,  Jeanne Stuckey 2,  Shaomeng Wang 1
Affiliations

Affiliations

  • 1 Comprehensive Cancer Center and Departments of Internal Medicine, Pharmacology and Medicinal Chemistry, University of Michigan, 1500 E. Medical Center Drive, Ann Arbor, MI 48109-0934, USA.
  • 2 Life Sciences Institute, University of Michigan, 1500 E. Medical Center Drive, Ann Arbor, MI 48109-0934, USA.
  • # Contributed equally.
PMID: 23448298 DOI: 10.1021/jm4001105
Abstract

Our previously reported Bcl-2/Bcl-xL Inhibitor, 4, effectively inhibited tumor growth but failed to achieve complete regression in vivo. We have now performed extensive modifications on its pyrrole core structure, which has culminated in the discovery of 32 (BM-1074). Compound 32 binds to Bcl-2 and Bcl-xL proteins with K(i) values of <1 nM and inhibits Cancer cell growth with IC50 values of 1-2 nM in four small-cell lung Cancer cell lines sensitive to potent and specific Bcl-2/Bcl-xL inhibitors. Compound 32 is capable of achieving rapid, complete, and durable tumor regression in vivo at a well-tolerated dose schedule. Compound 32 is the most potent and efficacious Bcl-2/Bcl-xL Inhibitor reported to date.

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