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, 7620 NW Loop 410, San Antonio, TX 78245-0549, USA.
Steroids. 2008 Feb;73(2):171-83. doi: 10.1016/j.steroids.2007.10.016. Epub 2007 Nov 17.
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 17beta-hydroxy function. Of nine analogs synthesized, five have demonstrated superior antiproliferative activities compared to 2-methoxyestradiol.
描述了几种新型2-甲氧基雌二醇类似物的合成及其抗有丝分裂活性。结构修饰包括D环同系化、将六元D环芳构化为柯因型分子、在五元D环中引入不饱和键以及用烷基和乙炔基取代17β-羟基官能团。在合成的九种类似物中，有五种表现出比2-甲氧基雌二醇更强的抗增殖活性。
