4.5 Article

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

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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 21, 页码 6241-6244

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.08.020

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Antitumor; Antiproliferative; 2-Methoxyestradiol analogs

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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 anti-proliferative 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. (C) 2009 Elsevier Ltd. All rights reserved.

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