Title of article
Rational design of conformationally restricted quinazolinone inhibitors of poly(ADP-ribose)polymerase
Author/Authors
Kouji Hattori، نويسنده , , Yoshiyuki Kido، نويسنده , , Hirofumi Yamamoto، نويسنده , , Junya Ishida، نويسنده , , Akinori Iwashita، نويسنده , , Kayoko Mihara، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
5
From page
5577
To page
5581
Abstract
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.
Keywords
Poly(ADP-ribose)polymerase PARP-1 , x-ray , SBDD , Conformationally restricted , Quinazolinone
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798657
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