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.
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DOI：
10.1016/j.bmc.2015.03.024
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发表时间：
2015-05
影响因子：
3.5
通讯作者：
Yichao Wan;Shaolei Wu;Guizhi Xiao;Tingting Liu;Xuben Hou;Cheng Chen;Peng Guan;Xinying Yang;
中科院分区：
文献类型：
--
作者：
Yichao Wan;Shaolei Wu;Guizhi Xiao;Tingting Liu;Xuben Hou;Cheng Chen;Peng Guan;Xinying Yang;
B细胞淋巴瘤-2（Bcl-2）蛋白是癌症治疗的有希望的靶点。本论文设计并合成了一系列2-硫代-4-噻唑烷酮类化合物作为Bcl-2抑制剂。它们中的大多数对抗凋亡Bcl-2蛋白具有良好的抑制活性。其中化合物31对K562的生长抑制作用与（R）-棉酚相似。此外，它抑制髓细胞白血病序列1（Mcl-1）蛋白，aKi值为74 nM。
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, compound31has similar growth inhibition towards K562 compared to (R)-Gossypol. In addition, it inhibits the myeloid cell leukemia sequence 1 (Mcl-1) protein with aKivalue of 74 nM.