Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors
Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors
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DOI：
10.1021/jm0255769
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发表时间：
2003-01-16
影响因子：
7.3
通讯作者：
Golding, BT
中科院分区：
文献类型：
--
作者：
Skalitzky, DJ;Marakovits, JT;Golding, BT
合成了新型三环苯并咪唑甲酰胺聚（ADP-核糖）聚合酶-1（PARP-1）抑制剂。发现几种化合物是替莫唑胺和拓扑替康在A549和LoVo细胞系中的强效化学增强剂。通过直接测量化学诱导的DNA损伤引起的NAD（+）消耗和AD聚核糖聚合物形成，证实了PARP-1的体外抑制作用。
Novel tricyclic benzimidazole carboxamide poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors have been synthesized. Several compounds were found to be powerful chemopotentiators of temozolomide and topotecan in both A549 and LoVo cell lines. In vitro inhibition of PARP-1 was confirmed by direct measurement of NAD(+) depletion and ADPribose polymer formation caused by chemically induced DNA damage.