کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1369449 | 981779 | 2012 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of novel dihydroimidazothiazole derivatives as p53–MDM2 protein–protein interaction inhibitors: Synthesis, biological evaluation and structure–activity relationships
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
Starting with Nutlins as an initial lead, we designed and generated bicyclic scaffolds aiming to place cis-bischlorophenyl moiety at the equivalent location where the hydrophobic interaction with MDM2 could be expected. As a result, we discovered novel MDM2 inhibitors possessing a dihydroimidazothiazole scaffold. Further exploration of the side chains on the dihydroimidazothiazole scaffold aided by molecular modeling resulted in compounds exhibiting almost comparable in vitro potency to Nutlin-3a.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 20, 15 October 2012, Pages 6338–6342
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 20, 15 October 2012, Pages 6338–6342
نویسندگان
Masaki Miyazaki, Haruko Kawato, Hiroyuki Naito, Masahiro Ikeda, Masaya Miyazaki, Mayumi Kitagawa, Takahiko Seki, Setsuko Fukutake, Masashi Aonuma, Tsunehiko Soga,