Design and synthesis of poly (ADP-ribose) polymerase-1 (PARP-1) inhibitors. Part 4: biological evaluation of imidazobenzodiazepines as potent PARP-1 inhibitors for …

…, M Ginski, S Lautar, K Lee-Wisdom, S Liang…

Index: Ferraris, Dana; Ficco, Rica Pargas; Dain, David; Ginski, Mark; Lautar, Susan; Lee-Wisdom, Kathy; Liang, Shi; Lin, Qian; Lu, May X.-C.; Morgan, Lisa; Thomas, Bert; Williams, Lawrence R.; Zhang, Jie; Zhou, Yinong; Kalish, Vincent J. Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 17 p. 3695 - 3707

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Citation Number: 59

Abstract

A class of poly (ADP-ribose) polymerase (PARP-1) inhibitors, the imidazobenzodiazepines, are presented in this text. Several derivatives were designed and synthesized with ionizable groups (ie, tertiary amines) in order to promote the desired pharmaceutical characteristics for administration in ischemic injury. Within this series, several compounds have excellent in vitro potency and our computational models accurately justify the structure–activity ...