Design and synthesis of poly (ADP-ribose) polymerase-1 (PARP-1) inhibitors. Part 3: In vitro evaluation of 1, 3, 4, 5-tetrahydro-benzo [c][1, 6]-and [c][1, 7]-naphthyridin- …

D Ferraris, RP Ficco, T Pahutski, S Lautar…

文献索引：Ferraris, Dana; Ficco, Rica Pargas; Pahutski, Thomas; Lautar, Susan; Huang, Shirley; Zhang, Jie; Kalish, Vincent Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 15 p. 2513 - 2518

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被引用次数: 25

摘要

The 1, 3, 4, 5-tetrahydro-benzo [c][1, 6]-and [c][1, 7]-napthyridin-6-ones are presented as a potent class of PARP-1 inhibitors. Derivatives of these partially saturated aza-5 [H]- phenanthridin-6-ones were designed and synthesized with tertiary amines for salt formation, thus enhancing aqueous solubility, iv formulation and their potential use in acute ischemic injuries (ie, myocardial ischemia and stroke). We found that partial saturation of the C-ring ...