کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1371059 | 981838 | 2011 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
2,4-Diaminopyrimidine inhibitors of c-Met kinase bearing benzoxazepine anilines
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Elaboration of the SAR around a series of 2,4-diaminopyrimidines led to a number of c-Met inhibitors in which kinase selectivity was modulated by substituents appended on the C4-aminobenzamide ring and the nature of the C2-aminoaryl ring. Further lead optimization of the C2-aminoaryl group led to benzoxazepine analogs whose pharmaceutical properties were modulated by the nature of the substituent on the benzoxazepine nitrogen. Tumor stasis (with partial regressions) were observed when an orally bioavailable analog was evaluated in a GTL-16 tumor xenograft mouse model. Subsequent PK/PD studies suggested that a metabolite contributed to the overall in vivo response.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 2, 15 January 2011, Pages 660–663
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 2, 15 January 2011, Pages 660–663
نویسندگان
Craig A. Zificsak, Jay P. Theroff, Lisa D. Aimone, Mark S. Albom, Thelma S. Angeles, Rebecca A. Brown, Deborah Galinis, Jennifer V. Grobelny, Torsten Herbertz, Jean Husten, Laura S. Kocsis, Christine LoSardo, Sheila J. Miknyoczki, Seetha Murthy,