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作为Mcl-1和Bcl-x(L)与Bim结合的破坏剂的环状海生吡咯衍生物

Cyclic marinopyrrole derivatives as disruptors of Mcl-1 and Bcl-x(L) binding to Bim.

作者信息

Cheng Chunwei, Liu Yan, Balasis Maria E, Simmons Nicholas L, Li Jerry, Song Hao, Pan Lili, Qin Yong, Nicolaou K C, Sebti Said M, Li Rongshi

机构信息

Key Laboratory of Drug Targeting and Drug Delivery Systems of the Ministry of Education and State Key Laboratory of Biotherapy, Department of Medicinal Natural Products, West China School of Pharmacy, Sichuan University, Chengdu 610041, China.

Chemical Biology & Molecular Medicine Program, Department of Drug Discovery, H. Lee Moffitt Cancer Center and Research Institute, 12902 Magnolia Drive, Tampa, FL 33612, USA.

出版信息

Mar Drugs. 2014 Mar 7;12(3):1335-48. doi: 10.3390/md12031335.

DOI:10.3390/md12031335
PMID:24608970
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3967213/
Abstract

A series of novel cyclic marinopyrroles were designed and synthesized. Their activity to disrupt the binding of the pro-apoptotic protein, Bim, to the pro-survival proteins, Mcl-1 and Bcl-x(L), was evaluated using ELISA assays. Both atropisomers of marinopyrrole A (1) show similar potency. A tetrabromo congener 9 is two-fold more potent than 1. Two novel cyclic marinopyrroles (3 and 4) are two- to seven-fold more potent than 1.

摘要

设计并合成了一系列新型环状海环吡咯。使用酶联免疫吸附测定（ELISA）分析评估了它们破坏促凋亡蛋白Bim与促生存蛋白Mcl-1和Bcl-x(L)结合的活性。海环吡咯A（1）的两种阻转异构体显示出相似的效力。一种四溴同系物9的效力比1高两倍。两种新型环状海环吡咯（3和4）的效力比1高两到七倍。

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本文引用的文献

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A novel small-molecule inhibitor of mcl-1 blocks pancreatic cancer growth in vitro and in vivo.一种新型的Mcl-1小分子抑制剂在体外和体内均能抑制胰腺癌生长。
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Mar Drugs. 2014 Jul 29;12(8):4311-25. doi: 10.3390/md12084311.
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Marinopyrrole derivatives as potential antibiotic agents against methicillin-resistant Staphylococcus aureus (III).作为抗耐甲氧西林金黄色葡萄球菌潜在抗生素的海洋吡咯衍生物（III）。
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