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Design, synthesis and preliminary biological studies of pyrrolidine derivatives as Mcl-1 inhibitors

文献类型： 外文期刊

作者： Wan, Yichao 1 ; Wang, Junhua 2 ; Sun, Feng'e 1 ; Chen, Minglu 1 ; Hou, Xuben 1 ; Fang, Hao 1 ;

作者机构： 1.Shandong Univ, Minist Educ, Sch Pharm, Dept Med Chem,Key Lab Chem Biol, Jinan 250012, Shandong, Peoples R China

2.Shandong Acad Agr Sci, Inst Agrofood Sci & Technol, Jinan 250100, Shandong, Peoples R China

关键词： Apoptosis;Bcl-2;Mcl-1;Pyrrolidine;Anti-tumor

期刊名称：BIOORGANIC & MEDICINAL CHEMISTRY （ 影响因子：3.641； 五年影响因子：3.319 ）

ISSN：

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收录情况： SCI

摘要： Anti-apoptotic proteins, such as B-cell lymphoma (Bcl-2) protein, myeloid cell leukemia sequence 1 (Mcl-1) protein, are potential targets for cancer treatment. In the studies, a series of pyrrolidine derivatives were developed as potent Mcl-1 inhibitors. The preliminary biological studies suggested that most of target compounds exhibit good abilities for targeting Mcl-1 protein. Among them, compound 21 (K-i = 0.53 mu M) exhibited equal inhibitory activities towards Mcl-1 protein compared to positive control gossypol (K-i = 0.39 mu M). This compound also possessed good antiproliferative activities against MDA-MB-231 and PC-3 cancer cells. (c) 2015 Elsevier Ltd. All rights reserved.

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