- Design and synthesis of 2-(4,5,6,7-tetrahydrothienopyridin-2-yl)-benzoimidazole carboxamides as novel orally efficacious Poly(ADP-ribose)polymerase (PARP) inhibitors.
Design and synthesis of 2-(4,5,6,7-tetrahydrothienopyridin-2-yl)-benzoimidazole carboxamides as novel orally efficacious Poly(ADP-ribose)polymerase (PARP) inhibitors.
European journal of medicinal chemistry (2018-01-18)
Xuxing Chen, Xiajuan Huan, Qiufeng Liu, Yuqin Wang, Qian He, Cun Tan, Yi Chen, Jian Ding, Yechun Xu, Zehong Miao, Chunhao Yang
PMID29335205
RESUMEN
The nuclear protein poly(ADP-ribose) polymerases-1/2 (PARP-1/2) are involved in DNA repair damaged by endogenous or exogenous process. And PARP-1/2 inhibitors have been proved to be clinically efficacious for DNA repair deficient tumors in the past decade. We have developed a series of 4,5,6,7-tetrahydrothienopyridin-2-yl benzimidazole carboxamides as novel and potent PARP-1/2 inhibitors. The best compound resulted from this series is compound 27 which displays excellent PARP-1 and PARP-2 inhibitory activity with IC
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Discovery® C8 Supelguard Guard Cartridge Kit, 5 μm particle size, L × I.D. 2 cm × 4 mm, contains 2 nuts, 2 ferrules, 5cm tubing, 1 guard cartridge and 1 guard holder