Synthesis, antiproliferative, and pharmacokinetic properties of 3- and 17-double-modified analogs of 2-methoxyestradiol
作者： Gregory E. Agoston , Jamshed H. Shah , Lita Suwandi , Arthur D. Hanson , Xiaoguo Zhan
DOI: 10.1016/J.BMCL.2009.08.020
关键词:
摘要: The syntheses of 21 analogs 2-methoxyestradiol are presented, including ENMD-1198 which was selected for advancement into Phase 1 clinical trials in oncology. These were evaluated antiproliferative activity using breast tumor MDA-MB-231 cells, antiangiogenic HUVEC proliferation assays, and estrogenic MCF-7 cell proliferation. most active iv oral pharmacokinetic properties via cassette dosing rat mice models.
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