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WANG Lei, MA Jun, GU Mengyue, DI Rongrong, LIU Yu, LAI Yisheng. Design, synthesis and biological evaluation of five-membered heterocyclopyrimidines as MTH1 inhibitors[J]. Journal of China Pharmaceutical University, 2018, 49(4): 407-412. DOI: 10.11665/j.issn.1000-5048.20180404
Citation: WANG Lei, MA Jun, GU Mengyue, DI Rongrong, LIU Yu, LAI Yisheng. Design, synthesis and biological evaluation of five-membered heterocyclopyrimidines as MTH1 inhibitors[J]. Journal of China Pharmaceutical University, 2018, 49(4): 407-412. DOI: 10.11665/j.issn.1000-5048.20180404
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Design, synthesis and biological evaluation of five-membered heterocyclopyrimidines as MTH1 inhibitors

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  • 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.
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