The discovery and synthesis of novel adenosine substituted 2,3-dihydro-1H-isoindol-1-ones: potent inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1)

Jagtap, P., Southan, G.J., Baloglu, E., Ram, E., Mabley, J.G., Marton, A., Salzman, A.L. and Szabo, C. (2004) The discovery and synthesis of novel adenosine substituted 2,3-dihydro-1H-isoindol-1-ones: potent inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1) Bioorganic & medicinal chemistry letters, 14 . pp. 81-85. ISSN 0960-894X

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Abstract

A series of novel 4-(N-acyl)-2,3-dihydro-1H-isoindol-1-ones have been prepared from methyl-3-nitro-2-methylbenzoate and linked through various spacers to the adenosine derivatives 11 and 12. We found that potent inhibition of poly(ADP-ribose)polymerase-1 (PARP-1) was achieved when isoindolinone was linked to adenosine by a spacer group of a specific length. Introduction of piperazine and succinyl linkers between the isoindolinone and adenosine core structures resulted in highly potent compounds 8a and 10b, which showed IC50 values of 45 and 100 nM, respectively.

Item Type:Journal article
Subjects:B000 Health Professions > B200 Pharmacology Toxicology and Pharmacy
DOI (a stable link to the resource):10.1016/j.bmcl.2003.10.007
Faculties:Faculty of Science and Engineering > School of Pharmacy and Biomolecular Sciences > Chemical Biology
ID Code:193
Deposited By:editor spbs
Deposited On:21 Nov 2006
Last Modified:24 May 2013 11:58

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