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Bioorg Med Chem Lett. 2007 Oct 15;17(20):5577-81. Epub 2007 Aug 22.

Rational design of conformationally restricted quinazolinone inhibitors of poly(ADP-ribose)polymerase.

Author information

1
Chemistry Research Laboratories, Astellas Pharma Inc., 21 Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan. kouji.hattori@jp.astellas.com

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 IC(50)=8.7 nM and good brain penetration.

PMID:
17804225
DOI:
10.1016/j.bmcl.2007.07.091
[Indexed for MEDLINE]

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