کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1358007 981307 2014 9 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy
چکیده انگلیسی

The field of small-molecule inhibitors of protein–protein interactions is rapidly advancing and the specific area of inhibitors of the p53/MDM2 interaction is a prime example. Several groups have published on this topic and multiple compounds are in various stages of clinical development. Building on the strength of the discovery of RG7112, a Nutlin imidazoline-based compound, and RG7388, a pyrrolidine-based compound, we have developed additional scaffolds that provide opportunities for future development. Here, we report the discovery and optimization of a highly potent and selective series of spiroindolinone small-molecule MDM2 inhibitors, culminating in RO8994.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 22, Issue 15, 1 August 2014, Pages 4001–4009
نویسندگان
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