Release Time:2019-03-09  Hits:

Indexed by: Journal Article

Date of Publication: 2014-11-01

Journal: BIOORGANIC & MEDICINAL CHEMISTRY

Included Journals: Scopus、PubMed、SCIE

Volume: 22

Issue: 21

Page Number: 5738-5746

ISSN: 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.