کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1375162 | 981933 | 2006 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Kinesin spindle protein (KSP) inhibitors. Part 2: The design, synthesis, and characterization of 2,4-diaryl-2,5-dihydropyrrole inhibitors of the mitotic kinesin KSP
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Kinesin spindle protein (KSP) inhibitors. Part 2: The design, synthesis, and characterization of 2,4-diaryl-2,5-dihydropyrrole inhibitors of the mitotic kinesin KSP Kinesin spindle protein (KSP) inhibitors. Part 2: The design, synthesis, and characterization of 2,4-diaryl-2,5-dihydropyrrole inhibitors of the mitotic kinesin KSP](/preview/png/1375162.png)
چکیده انگلیسی
The evolution of 2,4-diaryl-2,5-dihydropyrroles as inhibitors of KSP is described. Introduction of basic amide and urea moieties to the dihydropyrrole nucleus enhanced potency and aqueous solubility, simultaneously, and provided compounds that caused mitotic arrest of A2780 human ovarian carcinoma cells with EC50s < 10 nM. Ancillary hERG activity was evaluated for this series of inhibitors.
2,4-Diaryl-2,5-dihydropyrroles are reported as potent inhibitors of the mitotic kinesin KSP.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 7, 1 April 2006, Pages 1775–1779
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 7, 1 April 2006, Pages 1775–1779
نویسندگان
Mark E. Fraley, Robert M. Garbaccio, Kenneth L. Arrington, William F. Hoffman, Edward S. Tasber, Paul J. Coleman, Carolyn A. Buser, Eileen S. Walsh, Kelly Hamilton, Christine Fernandes, Michael D. Schaber, Robert B. Lobell, Weikang Tao,