聚ADP核糖聚合酶
化学
三环
聚合酶
苯并咪唑
核糖
NAD+激酶
体外
立体化学
生物化学
酶
有机化学
作者
Donald J. Skalitzky,Joseph Marakovits,Karen A. Maegley,Anne Ekker,Xin Yu,Zdeněk Hostomský,S. E. Webber,Brian Eastman,Robert J. Almassy,Jianke Li,Nicola J. Curtin,David R. Newell,A. Hilary Calvert,Roger J. Griffin,Bernard T. Golding
摘要
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 ADP-ribose polymer formation caused by chemically induced DNA damage.
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