|
|||||
|
|
Synthesis and biological evaluation of piperidyl benzimidazole carboxamide derivatives as potent PARP-1 inhibitors and antitumor agents |
|
| Authors: | Xinwei Zhang Cunlong Zhang Lin Tang Kuan Lu Huan Zhao Weibin Wu Yuyang Jiang |
| Institution: | Department of Chemistry;The State Key Laboratory of Chemical Oncogenomics;Shenzhen Kivita Innovative Drug Discovery Institute;Shenzhen Ruikang Pharmaceutical Technology Co.;Department of Pharmacology and Pharmaceutical Sciences |
| Abstract: | We have synthesized a series of compounds based on a piperidyl benzimidazole carboxamide structure, and tested their PARP-1 inhibitory activity, as well as cellular inhibitory activity. Some of them show great potency as PARP-1 inhibitors and antitumor activity, which are valuable for further research. In addition, the predicted ADME properties and proposed binding mode with PARP-1 of the compounds were obtained via computational simulation. |
| Keywords: | PARP-1 inhibitor Piperidyl benzimidazole carboxamide A-620223 Structure-activity relationship Antitumor activity |
| 本文献已被 CNKI 维普 ScienceDirect 等数据库收录！ | |
| 点击此处可从《中国化学快报》浏览原始摘要信息 | |
| 点击此处可从《中国化学快报》下载免费的PDF全文 | |