کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1372909 | 981885 | 2009 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis, antiproliferative, and pharmacokinetic properties of 3- and 17-double-modified analogs of 2-methoxyestradiol
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Synthesis, antiproliferative, and pharmacokinetic properties of 3- and 17-double-modified analogs of 2-methoxyestradiol Synthesis, antiproliferative, and pharmacokinetic properties of 3- and 17-double-modified analogs of 2-methoxyestradiol](/preview/png/1372909.png)
چکیده انگلیسی
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.
A series of doubly modified analogs of 2-methoxyestradiol were designed, synthesized and evaluated for antiproliferative, antiangiogenic, estrogenic and pharmacokinetic properties.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 21, 1 November 2009, Pages 6241–6244
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 21, 1 November 2009, Pages 6241–6244
نویسندگان
Gregory E. Agoston, Jamshed H. Shah, Lita Suwandi, Arthur D. Hanson, Xiaoguo Zhan, Theresa M. LaVallee, Victor Pribluda, Anthony M. Treston,