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Updated: Jun 20, 2026

An In Vivo Estrogen Deficiency Mouse Model for Screening Exogenous Estrogen Treatments of Cardiovascular Dysfunction After Menopause
Published on: August 13, 2019
Synthesis, antiproliferative, and pharmacokinetic properties of 3- and 17-double-modified analogs of
Gregory E Agoston1, Jamshed H Shah, Lita Suwandi
1EntreMed, Inc., 9640 Medical Center Drive, Rockville, MD 20850, USA.
Abstract:
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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