2. Academic Validation
  3. Design, synthesis and preliminary bioactivity studies of 2-thioxo-4-thiazolidinone derivatives as Bcl-2 inhibitors

Design, synthesis and preliminary bioactivity studies of 2-thioxo-4-thiazolidinone derivatives as Bcl-2 inhibitors

  • Bioorg Med Chem. 2015 May 1;23(9):1994-2003. doi: 10.1016/j.bmc.2015.03.024.
Yichao Wan 1,  Shaolei Wu 1,  Guizhi Xiao 1,  Tingting Liu 1,  Xuben Hou 1,  Chen Chen 1,  Peng Guan 1,  Xinying Yang 1,  Hao Fang 2
Affiliations

Affiliations

  • 1 Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmacy, Shandong University, 44 West Wenhua Road, Jinan, Shandong 250012, PR China.
  • 2 Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmacy, Shandong University, 44 West Wenhua Road, Jinan, Shandong 250012, PR China. Electronic address: haofangcn@sdu.edu.cn.
PMID: 25818766 DOI: 10.1016/j.bmc.2015.03.024
Abstract

The B-cell lymphoma-2 (Bcl-2) protein is a promising target for Cancer therapy. In the present study, a series of 2-thioxo-4-thiazolidinone derivatives were designed and synthesized as Bcl-2 inhibitors. Most of them possessed decent inhibitory activity for anti-apoptotic Bcl-2 proteins. Among them, compound 31 has similar growth inhibition towards K562 compared to (R)-Gossypol. In addition, it inhibits the myeloid cell leukemia sequence 1 (Mcl-1) protein with a Ki value of 74 nM.

Keywords

2-Thioxo-4-thiazolidinone; Anti-tumor; Bcl-2; Inhibitors.

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