Solid phase-assisted synthesis and screening of a small library of N-(4-hydroxyphenyl)retinamide (4-HPR) analogs

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:17

Article

Mershon, Serena M. ; Anding, Allyson L. ; Chapman, Jason S. ; Clagett-Dame, Margaret ; Stonerock, Laura A. ; Curley, Robert W., Jr.

关键词: library;    solid phase synthesis;    retinoid;    4-HPR;    mammary tumor cell;    chemoprevention;   

DOI  :  10.1016/j.bmcl.2006.10.050

来源: Elsevier

【 摘 要 】

Using solid phase-assisted synthesis and purification, a 49 member library of analogs of the main mammary tumor chemopreventive retinoid N-(4-hydroxyphenyl)retinamide (4-HPR) has been prepared. After prescreening for growth inhibitory activity in human mammary tumor cells (MCF-7) in culture, most of those analogs which showed activity (12 of them) were assayed for apoptosis-inducing activity in the MCF-7 cells. At least 3 of the analogs (13, 24, and 28) showed activity approaching that of 4-HPR. (c) 2006 Elsevier Ltd. All rights reserved.

【 授权许可】

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