A series of imidazo[4,5-c]pyridine-7-carboxamide derivatives as poly(ADP-ribose) polymerase (PARP) inhibitors have been developed. All target compounds were evaluated for their PARP-1 inhibitory activity and some were further assessed for cellular potency. These efforts led to identification of a novel PARP-1 inhibitor 2-(1-propylpiperidin-4-yl)-3H-imidazo[4,5-c]pyridine-7-carboxamide 11a (XZ-120312). 11a displayed strong inhibition against the PARP-1 enzyme with an IC50 of 8.6±0.6 nM and excellent potentiation of temozolomide cytotoxicity in cancer cell lines SW-620, MDA-MB-468 and A549 by 4.0, 3.0 and 7.7 times, respectively.

中文翻译：

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2-（1-丙基哌啶-4-基）-3H-咪唑并[4,5-c]吡啶-7-羧酰胺的发现和合成孔径雷达研究：一种有效的聚（ADP-核糖）聚合酶-1（PARP-1抑制剂） ）用于治疗癌症。

已经开发了一系列作为聚（ADP-核糖）聚合酶（PARP）抑制剂的咪唑并[4,5-c]吡啶-7-羧酰胺衍生物。评价所有靶标化合物的PARP-1抑制活性，并进一步评价一些靶标的细胞效力。这些努力导致鉴定了新型的PARP-1抑制剂2-（1-丙基哌啶-4-基）-3H-咪唑并[4，5-c]吡啶-7-羧酰胺11a（XZ-120312）。图11a显示了对PARP-1酶的强抑制，IC50为8.6±0.6nM，并且在癌细胞系SW-620，MDA-MB-468和A549中替莫唑胺细胞毒性的优异增强分别为4.0、3.0和7.7倍。