Design, Synthesis, Biological Evaluation, and Molecular Docking Studies of Thiazolidine-2,4-dione Derivatives as Mcl-1 Inhibitors

被引：2

作者：

Deng, Xu ^{[1
]}

Long, Jiabing ^{[1
]}

Wang, Wenyan ^{[1
]}

Xia, Shen ^{[1
]}

Wan, Yichao ^{[1
,2
]}

机构：

[1] Hunan Univ Sci & Technol, Sch Chem & Chem Engn, Minist Educ, Key Lab Theoret Organ Chem & Funct Mol, Xiangtan 411201, Hunan, Peoples R China

[2] Hunan Univ Sci & Technol, Hunan Prov Key Lab Adv Mat New Energy Storage & C, Hunan Prov Key Lab Controllable Preparat & Funct, Xiangtan 411201, Hunan, Peoples R China

来源：

RUSSIAN JOURNAL OF GENERAL CHEMISTRY | 2022年 / 92卷 / 03期

基金：

中国国家自然科学基金;

关键词：

Mcl-1; inhibitors; thiazolidine-2; 4-dione; anti-cancer; scaffold hopping; DISCOVERY;

D O I：

10.1134/S1070363222030148

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

In the study, two series of thiazolidine-2,4-dione derivatives have been designed, synthesized and evaluated for their inhibitory activity of Mcl-1 protein by fluorescence polarization assays (FPAs). Among those, the most potent product has demonstrated inhibitory activity against Mcl-1 (inhibitory rate 94% at 10 mu M) higher than that of the positive control WL-276 (90%).

引用

页码：464 / 469

页数：6

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