کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1358021 | 981307 | 2014 | 16 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
In the last decade the heat shock protein 90 (Hsp90) has emerged as a major therapeutic target and many efforts have been dedicated to the discovery of Hsp90 inhibitors as new potent anticancer agents. Here we report the identification of a novel class of Hsp90 inhibitors by means of a biophysical FAXS-NMR based screening of a library of fragments. The use of X-ray structure information combined with modeling studies enabled the fragment evolution of the initial triazoloquinazoline hit to a class of compounds with nanomolar potency and drug-like properties suited for further lead optimization.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 22, Issue 15, 1 August 2014, Pages 4135–4150
Journal: Bioorganic & Medicinal Chemistry - Volume 22, Issue 15, 1 August 2014, Pages 4135–4150
نویسندگان
Elena Casale, Nadia Amboldi, Maria Gabriella Brasca, Dannica Caronni, Nicoletta Colombo, Claudio Dalvit, Eduard R. Felder, Gianpaolo Fogliatto, Arturo Galvani, Antonella Isacchi, Paolo Polucci, Laura Riceputi, Francesco Sola, Carlo Visco, Fabio Zuccotto,