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Bioorg Med Chem Lett. 2009 Nov 1;19(21):6241-4. doi: 10.1016/j.bmcl.2009.08.020. Epub 2009 Aug 8.

Synthesis, antiproliferative, and pharmacokinetic properties of 3- and 17-double-modified analogs of 2-methoxyestradiol.

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  • 1EntreMed, Inc., 9640 Medical Center Drive, Rockville, MD 20850, USA.


The syntheses of 21 analogs of 2-methoxyestradiol are presented, including ENMD-1198 which was selected for advancement into Phase 1 clinical trials in oncology. These analogs were evaluated for antiproliferative activity using breast tumor MDA-MB-231 cells, for antiangiogenic activity in HUVEC proliferation assays, and for estrogenic activity in MCF-7 cell proliferation. The most active analogs were evaluated for iv and oral pharmacokinetic properties via cassette dosing in rat and in mice pharmacokinetic models.

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