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N-(4-羟基苯基)视黄酰胺（4-HPR）类似物的小型文库的固相辅助合成与筛选。

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

作者信息

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

机构信息

Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA.

出版信息

Bioorg Med Chem Lett. 2007 Feb 1;17(3):836-40. doi: 10.1016/j.bmcl.2006.10.050. Epub 2006 Oct 25.

DOI:10.1016/j.bmcl.2006.10.050
PMID:17112722
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1885232/
Abstract

Using solid phase-assisted synthesis and purification, a 49 member library of analogs of the 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.

摘要

采用固相辅助合成和纯化方法，制备了一个包含49个成员的乳腺肿瘤化学预防类视黄醇N-(4-羟基苯基)视黄酰胺(4-HPR)类似物库。在对培养的人乳腺肿瘤细胞(MCF-7)进行生长抑制活性预筛选后，对大多数显示出活性的类似物(其中12个)进行了MCF-7细胞凋亡诱导活性检测。至少有3个类似物(13、24和28)显示出接近4-HPR的活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48fb/1885232/09202520d8b2/nihms16892f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48fb/1885232/a1c25ac30b8a/nihms16892f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48fb/1885232/2fae604e189b/nihms16892f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48fb/1885232/09202520d8b2/nihms16892f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48fb/1885232/a1c25ac30b8a/nihms16892f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48fb/1885232/2fae604e189b/nihms16892f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48fb/1885232/09202520d8b2/nihms16892f3.jpg

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