Synthesis and antitumor activities of 3-modified 2-methoxyestradiol analogs.

Synthesis and antitumor activities of 3-modified 2-methoxyestradiol analogs.

Bioorganic & medicinal chemistry letters (2009-09-29)

Lita S Suwandi, Gregory E Agoston, Jamshed H Shah, Arthur D Hanson, Xiaoguo H Zhan, Theresa M Lavallee, Anthony M Treston

PMID19782568

摘要

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.