| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1365700 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
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.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Kouji Hattori, Yoshiyuki Kido, Hirofumi Yamamoto, Junya Ishida, Akinori Iwashita, Kayoko Mihara,