کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1365700 981570 2007 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Rational design of conformationally restricted quinazolinone inhibitors of poly(ADP-ribose)polymerase
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Rational design of conformationally restricted quinazolinone inhibitors of poly(ADP-ribose)polymerase
چکیده انگلیسی

A successful design of conformationally restricted novel quinazolinone derivatives linked via a cyclopentene moiety as potent poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors has been developed. One selected member of the new series, 8-chloro-2-[(3S)-3-(4-phenylpiperidin-1-yl)cyclopent-1-en-1-yl]quinazolin-4(3H)-one (S-16d), was found to be highly potent with IC50 = 8.7 nM and good brain penetration.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 20, 15 October 2007, Pages 5577–5581
نویسندگان
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