کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1365871 | 981575 | 2007 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Kinesin spindle protein (KSP) inhibitors. Part 6: Design and synthesis of 3,5-diaryl-4,5-dihydropyrazole amides as potent inhibitors of the mitotic kinesin KSP
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
3,5-Diaryl-4,5-dihydropyrazoles were discovered to be potent KSP inhibitors with excellent in vivo potency. These enzyme inhibitors possess desirable physical properties that can be readily modified by incorporation of a weakly basic amine. Careful adjustment of amine basicity was essential for preserving cellular potency in a multidrug resistant cell line while maintaining good aqueous solubility.
Dihydropyrazole amides such as 24 are potent inhibitors of KSP with favorable physical properties, pharmacokinetics, and in vivo potency. A diastereoselective synthesis of 24 is described.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 19, 1 October 2007, Pages 5390–5395
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 19, 1 October 2007, Pages 5390–5395
نویسندگان
Paul J. Coleman, John D. Schreier, Christopher D. Cox, Mark E. Fraley, Robert M. Garbaccio, Carolyn A. Buser, Eileen S. Walsh, Kelly Hamilton, Robert B. Lobell, Keith Rickert, Weikang Tao, Ronald E. Diehl, Vicki J. South, Joseph P. Davide, Nancy E. Kohl,