Synthesis and antimitotic activity of novel 2-methoxyestradiol analogs. Part III

被引：8

作者：

Rao, Pemmaraju N. ^{[1
]}

Cessac, James W. ^{[1
]}

Boyd, James W. ^{[1
]}

Hanson, Arthur D. ^{[2
]}

Shah, Jamshed ^{[2
]}

机构：

[1] SW Fdn Biomed Res, Dept Organ Chem, San Antonio, TX 78245 USA

[2] EntreMed Inc, Rockville, MD 20850 USA

来源：

STEROIDS | 2008年 / 73卷 / 02期

关键词：

estrogens; 2-methoxyestradiol; antiangiogenesis; antimitotic activity; antiproliferative activity;

D O I：

10.1016/j.steroids.2007.10.016

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The syntheses and antimitotic activity of several novel analogs of 2-methoxyestradiol are described. Structural modifications include ring-D homologation, aromatization of the six-membered ring-D to a chrysine type molecule, and introduction of unsaturation in five-membered ring-D along with substitution of alkyl and ethynyl groups for the 17 beta-hydroxy function. of nine analogs synthesized, five have demonstrated superior antiproliferative activities compared to 2-methoxyestradiol. (C) 2007 Elsevier Inc. All rights reserved.

引用

页码：171 / 183

页数：13

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