3-取代基 2-甲氧基雌二醇类似物的合成及抗肿瘤活性。
Synthesis and antitumor activities of 3-modified 2-methoxyestradiol analogs.
机构信息
EntreMed, Inc., 9640 Medical Center Drive, Rockville, MD 20850, USA.
出版信息
Bioorg Med Chem Lett. 2009 Nov 15;19(22):6459-62. doi: 10.1016/j.bmcl.2009.09.009. Epub 2009 Sep 9.
PMID:19782568
Abstract
The syntheses of 2-methoxyestradiol analogs with modifications at the 3-position are described. The analogs were assessed for their antiproliferative, antiangiogenic, and estrogenic activities. Several lead substituents were identified with similar or improved antitumor activities and reduced metabolic liability compared to 2-methoxyestradiol.
摘要
描述了 3 位取代基修饰的 2-甲氧基雌二醇类似物的合成。评估了类似物的抗增殖、抗血管生成和雌激素活性。与 2-甲氧基雌二醇相比，几种先导取代基具有相似或改善的抗肿瘤活性和降低的代谢风险。
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