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

  • Bioorg Med Chem Lett. 2009 Nov 15;19(22):6459-62. doi: 10.1016/j.bmcl.2009.09.009.
Lita S Suwandi  1 ,  Gregory E Agoston ,  Jamshed H Shah ,  Arthur D Hanson ,  Xiaoguo H Zhan ,  Theresa M Lavallee ,  Anthony M Treston
Affiliations
  • 1. EntreMed, Inc., 9640 Medical Center Drive, Rockville, MD 20850, USA.
PMID: 19782568 DOI: 10.1016/j.bmcl.2009.09.009
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.