Synthesis and evaluation of a new generation of orally efficacious benzimidazole-based poly (ADP-ribose) polymerase-1 (PARP-1) inhibitors as anticancer agents

…, J Leverson, X Liu, PA Marcotte, AM Olson…

Index: Tong, Yunsong; Bouska, Jennifer J.; Ellis, Paul A.; Johnson, Eric F.; Leverson, Joel; Liu, Xuesong; Marcotte, Patrick A.; Olson, Amanda M.; Osterling, Donald J.; Przytulinska, Magdalena; Rodriguez, Luis E.; Shi, Yan; Soni, Nirupama; Stavropoulos, Jason; Thomas, Sheela; Donawho, Cherrie K.; Frost, David J.; Luo, Yan; Giranda, Vincent L.; Penning, Thomas D. Journal of Medicinal Chemistry, 2009 , vol. 52, # 21 p. 6803 - 6813

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Citation Number: 58

Abstract

Small molecule inhibitors of PARP-1 have been pursued by various organizations as potential therapeutic agents either capable of sensitizing cytotoxic treatments or acting as stand-alone agents to combat cancer. As one of the strategies to expand our portfolio of PARP-1 inhibitors, we pursued unsaturated heterocycles to replace the saturated cyclic amine derivatives appended to the benzimidazole core. Not only did a variety of these ...