کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1360407 | 981434 | 2008 | 15 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Introduction of the 4-(4-bromophenyl)benzenesulfonyl group to hydrazide analogs of Ilomastat leads to potent gelatinase B (MMP-9) inhibitors with improved selectivity
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
Hydrazide derivatives of Ilomastat, carrying either aryl groups or distinct alkyl and arylsulfonyl moieties were synthesized and evaluated for their MMP inhibitory activity. Potent and selective MMP-9 inhibition (IC50 = 3 nM) was observed for compound 3m (arylsulfonyl group: 4-(4-Br–C6H4)–C6H4–SO2–). Interaction with the S2 enzyme subsite is mainly responsible for the inhibitory properties of this derivative as confirmed by molecular docking computation.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 16, Issue 18, 15 September 2008, Pages 8745–8759
Journal: Bioorganic & Medicinal Chemistry - Volume 16, Issue 18, 15 September 2008, Pages 8745–8759
نویسندگان
Gwennaël LeDour, Gautier Moroy, Matthieu Rouffet, Erika Bourguet, Dominique Guillaume, Martine Decarme, Haquima ElMourabit, Franck Augé, Alain J.P. Alix, Jean-Yves Laronze, Georges Bellon, William Hornebeck, Janos Sapi,