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
收藏
页码：171 / 183
页数：13
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