Design, synthesis and biological evaluation of five-membered heterocyclopyrimidines as MTH1 inhibitors
10.11665/j.issn.1000-5048.20180404
- VernacularTitle:五元杂环并嘧啶类MTH1抑制剂的设计、合成及生物活性评价
- Author:
Lei WANG
1
;
Jun MA
;
Mengyue GU
;
Rongrong DI
;
Yu LIU
;
Yisheng LAI
Author Information
1. 中国药科大学新药研究中心
- Publication Type:Journal Article
- Keywords:
five-membered heterocyclopyrimidine;
oxidative DNA damage;
DNA repair;
MTH1 inhibitor;
synthesis;
antitumor;
biological evaluation
- From:
Journal of China Pharmaceutical University
2018;49(4):407-412
- CountryChina
- Language:Chinese
-
Abstract:
Based on the reported inhibitors TH287, 17 five-membered heterocyclopyrimidine derivatives were designed and synthesized by cyclization, scaffold hopping, bioisosterism and molecular docking technology. The bioassays determined by malachite green method demonstrated that the target compounds displayed good inhibitory activity against MTH1. Among them, the IC50 value of 7 compounds was less than 1 μmol/L, suggesting that these compounds may be candidates for further investigation.
