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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.

    Agoston GE, Shah JH, Suwandi L, Hanson AD, Zhan X, LaVallee TM, Pribluda V, Treston AM.

    Source

    EntreMed, 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.

    PMID:
    19782564
    [PubMed - indexed for MEDLINE]

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