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Design, synthesis and structure-activity relationship studies of morpholino-1H-phenalene derivatives that antagonize Mcl-1/Bcl-2

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Indexed by:期刊论文

Date of Publication:2014-11-01

Journal:BIOORGANIC & MEDICINAL CHEMISTRY

Included Journals:SCIE、PubMed、Scopus

Volume:22

Issue:21

Page Number:5738-5746

ISSN No.:0968-0896

Key Words:Dual inhibitors; Hydrogen bond; Apoptosis; Mcl-1; Bcl-2

Abstract:We report herein characteristic studies of Mcl-1 and Bcl-2 dual inhibitors. It was found that a protruding carbonyl group forming hydrogen bond with R263 plays a predominant role compared with the hydrophobic group that occupies the p2 pocket. A series of dual inhibitors representing different parts of the morpholino-1H-phenalene were designed, synthesized and evaluated. (C) 2014 Elsevier Ltd. All rights reserved.

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