کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10591613 | 981757 | 2014 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Optimization beyond AMG 232: Discovery and SAR of sulfonamides on a piperidinone scaffold as potent inhibitors of the MDM2-p53 protein-protein interaction
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Optimization beyond AMG 232: Discovery and SAR of sulfonamides on a piperidinone scaffold as potent inhibitors of the MDM2-p53 protein-protein interaction Optimization beyond AMG 232: Discovery and SAR of sulfonamides on a piperidinone scaffold as potent inhibitors of the MDM2-p53 protein-protein interaction](/preview/png/10591613.png)
چکیده انگلیسی
We recently reported on the discovery of AMG 232, a potent and selective piperidinone inhibitor of the MDM2-p53 interaction. AMG 232 is being evaluated in human clinical trials for cancer. Continued exploration of the N-alkyl substituent of this series, in an effort to optimize interactions with the MDM2 glycine-58 shelf region, led to the discovery of sulfonamides such as compounds 31 and 38 that have similar potency, hepatocyte stability and rat pharmacokinetic properties to AMG 232.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 16, 15 August 2014, Pages 3782-3785
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 16, 15 August 2014, Pages 3782-3785
نویسندگان
Yingcai Wang, Jiang Zhu, Jiwen (Jim) Liu, Xiaoqi Chen, Jeff Mihalic, Jeffrey Deignan, Ming Yu, Daqing Sun, Frank Kayser, Lawrence R. McGee, Mei-Chu Lo, Ada Chen, Jing Zhou, Qiuping Ye, Xin Huang, Alexander M. Long, Peter Yakowec, Jonathan D. Oliner,