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Rational design of conformationally restricted quinazolinone inhibitors of poly(ADP-ribose)polymerase.
Bioorg Med Chem Lett. 2007 Oct 15; 17(20):5577-81.BM

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.

Authors+Show Affiliations

Hattori K
Chemistry Research Laboratories, Astellas Pharma Inc., 21 Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan. kouji.hattori@jp.astellas.com
Kido Y
No affiliation info available
Yamamoto H
No affiliation info available
Ishida J
No affiliation info available
Iwashita A
No affiliation info available
Mihara K
No affiliation info available

MeSH

AnimalsCattleCross-Linking ReagentsDrug DesignEnzyme InhibitorsMicrosomes, LiverMolecular ConformationMolecular StructurePoly(ADP-ribose) Polymerase InhibitorsPoly(ADP-ribose) PolymerasesQuinazolinonesStructure-Activity Relationship

Pub Type(s)

Journal Article

Language

eng

PubMed ID

17804225

Citation

Hattori, Kouji, et al. "Rational Design of Conformationally Restricted Quinazolinone Inhibitors of Poly(ADP-ribose)polymerase." Bioorganic & Medicinal Chemistry Letters, vol. 17, no. 20, 2007, pp. 5577-81.
Hattori K, Kido Y, Yamamoto H, et al. Rational design of conformationally restricted quinazolinone inhibitors of poly(ADP-ribose)polymerase. Bioorg Med Chem Lett. 2007;17(20):5577-81.
Hattori, K., Kido, Y., Yamamoto, H., Ishida, J., Iwashita, A., & Mihara, K. (2007). Rational design of conformationally restricted quinazolinone inhibitors of poly(ADP-ribose)polymerase. Bioorganic & Medicinal Chemistry Letters, 17(20), 5577-81.
Hattori K, et al. Rational Design of Conformationally Restricted Quinazolinone Inhibitors of Poly(ADP-ribose)polymerase. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5577-81. PubMed PMID: 17804225.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Rational design of conformationally restricted quinazolinone inhibitors of poly(ADP-ribose)polymerase. AU - Hattori,Kouji, AU - Kido,Yoshiyuki, AU - Yamamoto,Hirofumi, AU - Ishida,Junya, AU - Iwashita,Akinori, AU - Mihara,Kayoko, Y1 - 2007/08/22/ PY - 2007/03/29/received PY - 2007/07/27/revised PY - 2007/07/30/accepted PY - 2007/9/7/pubmed PY - 2007/12/13/medline PY - 2007/9/7/entrez SP - 5577 EP - 81 JF - Bioorganic & medicinal chemistry letters JO - Bioorg Med Chem Lett VL - 17 IS - 20 N2 - 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. SN - 0960-894X UR - https://www.unboundmedicine.com/medline/citation/17804225/Rational_design_of_conformationally_restricted_quinazolinone_inhibitors_of_poly_ADP_ribose_polymerase_ DB - PRIME DP - Unbound Medicine ER -