کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1377244 | 981974 | 2006 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
We have screened molecules for inhibition of MetAP2 as a novel approach toward antiangiogenesis and anticancer therapy using affinity selection/mass spectrometry (ASMS) employing MetAP2 loaded with Mn2+ as the active site metal. After a series of anthranilic acid sulfonamides with micromolar affinities was identified, chemistry efforts were initiated. The micromolar hits were quickly improved to potent nanomolar inhibitors by chemical modifications guided by insights from X-ray crystallography.
Synthesis and biological activity of novel methionine aminopeptidase type -2 inhibitors having a sulfonamide bond are reported.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 13, 1 July 2006, Pages 3574–3577
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 13, 1 July 2006, Pages 3574–3577
نویسندگان
Megumi Kawai, Nwe Y. BaMaung, Steve D. Fidanze, Scott A. Erickson, Jason S. Tedrow, William J. Sanders, Anil Vasudevan, Chang Park, Charles Hutchins, Kenneth M. Comess, Douglas Kalvin, Jieyi Wang, Qian Zhang, Pingping Lou, Lora Tucker-Garcia,