Bioorganic & medicinal chemistry

Synthesis of 3-substituted benzamides and 5-substituted isoquinolin-1 (2H)-ones and preliminary evaluation as inhibitors of poly (ADP-ribose) polymerase (PARP)

CY Watson, WJD Whish, MD Threadgill

Index: Watson, Corrine Y.; Whish, William J. D.; Threadgill, Michael D. Bioorganic and Medicinal Chemistry, 1998 , vol. 6, # 6 p. 721 - 734

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Citation Number: 73

Abstract

Inhibitors of poly (ADP-ribose) polymerase (PARP) inhibit repair of damaged DNA and thus potentiate radiotherapy and chemotherapy of cancer. 3-Substituted benzamides and 5- substituted isoquinolin-1-ones have been synthesised and evaluated for inhibition of PARP. Reduction of 3-(bromoacetyl) benzamide, followed by treatment with base, gave RS-3- oxiranylbenzamide. Reduction of 3-(hydroxyacetyl) benzonitrile with bakers' yeast gave ...