Rao Pemmaraju N, Cessac James W, Boyd James W, Hanson Arthur D, Shah Jamshed
Department of Organic Chemistry, Southwest Foundation for Biomedical Research, P.O. Box 760549, San Antonio, TX 78245-0549, USA.
Steroids. 2008 Feb;73(2):158-70. doi: 10.1016/j.steroids.2007.11.003. Epub 2007 Nov 22.
The syntheses and antimitotic activity of several novel 18a-homo-analogs of 2-methoxyestradiol are described. Structural modifications of the parent 2-methoxy-18a-homoestradiol include introduction of unsaturation in the D-ring and methylation of the 17-OH. Of seven analogs synthesized, one has demonstrated superior biological activities compared to 2-methoxyestradiol. The relationship between biological activity and the conformational preference of the 13-ethyl group as determined by computational analysis is discussed.
描述了几种新型2-甲氧基雌二醇的18α-高类似物的合成及抗有丝分裂活性。母体2-甲氧基-18α-高雌二醇的结构修饰包括在D环引入不饱和键和17-OH甲基化。在合成的七种类似物中，有一种已显示出比2-甲氧基雌二醇更优异的生物活性。讨论了通过计算分析确定的生物活性与13-乙基构象偏好之间的关系。
