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

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.

A lead-generation series of analogs of 2-methoxyestradiol modified at the 3-position were designed, synthesized and evaluated for antiproliferative, antiangiogenic, and estrogenic properties.Figure optionsDownload as PowerPoint slide