کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10587718 | 981436 | 2013 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
N-substituted azaindoles as potent inhibitors of Cdc7 kinase
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Cdc7 kinase is responsible for the initiation and regulation of DNA replication and has been proposed as a target for cancer therapy. We have identified a class of Cdc7 inhibitors based on a substituted indole core. Synthesis of focused indole and azaindole analogs yielded potent and selective 5-azaindole Cdc7 inhibitors with improved intrinsic metabolic stability (ie 36). In parallel, quantum mechanical conformational analysis helped to rationalize SAR observations, led to a proposal of the preferred binding conformation in the absence of co-crystallography data, and allowed the design of 7-azaindole 37 as a second lead in this series.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 7, 1 April 2013, Pages 2056-2060
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 7, 1 April 2013, Pages 2056-2060
نویسندگان
Marian C. Bryan, James R. Falsey, Mike Frohn, Andreas Reichelt, Guomin Yao, Michael D. Bartberger, Julie M. Bailis, Leeanne Zalameda, Tisha San Miguel, Elizabeth M. Doherty, John G. Allen,