4.7 Article

Design, synthesis and preliminary bioactivity studies of imidazolidine-2,4-dione derivatives as Bcl-2 inhibitors

Journal

BIOORGANIC & MEDICINAL CHEMISTRY
Volume 23, Issue 23, Pages 7359-7365

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2015.10.023

Keywords

Bcl-2; Imidazolidine-2,4-dione; Inhibitors; Antitumor

Funding

  1. National Natural Science Foundation of China [21172133]
  2. Shandong Natural Science Fund for Distinguished Young Scholars [JQ201319]
  3. Program for New Century Excellent Talents in University [NCET-12-0337]

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Anti-apoptotic B-cell lymphoma-2 (Bcl-2) proteins are promising targets for cancer therapy. In the present study, a series of imidazolidine-2,4-dione derivatives were designed and synthesized to test their inhibitory activities against anti-apoptotic Bcl-2 proteins. Among them, compound 8k had better growth inhibitory effects on K562 and PC-3 cell lines compared to lead compound WL-276. (C) 2015 Elsevier Ltd. All rights reserved.

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