کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1376900 | 981967 | 2008 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design and identification of selective HER-2 sheddase inhibitors via P1′ manipulation and unconventional P2′ perturbations to induce a molecular metamorphosis
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
In an effort to obtain a MMP selective and potent inhibitor of HER-2 sheddase (ADAM-10), the P1′ group of a novel class of (6S,7S)-7-[(hydroxyamino)carbonyl]-6-carboxamide-5-azaspiro[2.5]octane-5-carboxylates was attenuated and the structure–activity relationships (SAR) will be discussed. In addition, it was discovered that unconventional perturbation of the P2′ moiety could confer MMP selectivity, which was hypothesized to be a manifestation of the P2′ group effecting global conformational changes.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 1, 1 January 2008, Pages 159–163
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 1, 1 January 2008, Pages 159–163
نویسندگان
Wenqing Yao, Jincong Zhuo, David M. Burns, Yun-Long Li, Ding-Quan Qian, Colin Zhang, Chunhong He, Meizhong Xu, Eric Shi, Yanlong Li, Cindy A. Marando, Maryanne B. Covington, Gengjie Yang, Xiangdong Liu, Max Pan, Jordan S. Fridman, Peggy Scherle,