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

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Hattori K, Kido Y, Yamamoto H, Ishida J, Iwashita A, Mihara K

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

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

PubMed ID

17804225 [ View in PubMed

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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)-o ne (S-16d), was found to be highly potent with IC(50)=8.7 nM and good brain penetration.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
2-{3-[4-(4-Fluorophenyl)-3,6-Dihydro-1(2h)-Pyridinyl]Propyl}-8-Methyl-4(3h)-Quinazolinone	Poly [ADP-ribose] polymerase 1	IC 50 (nM)	8	N/A	N/A	Details