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Antiproliferative activity of ursolic acid/glycyrrhetinic acid-uracil/thymine hybrids

Journal 2019 · IF 1.72 · 28(6): 892-899 · 发表于 2019 年 4 月 16 日
作者: Sun Li,Chu Xiang-Wu,Liu Chun-mei,Sheng Li-Xin,Chen Zhuan-Xin,Cheng Ke-Guang
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摘要

As pharmacophore hybridization has been used frequently in the discovery of new drugs, ursolic acid/glycyrrhetinic acid-uracil/thymine hybrids have been synthesized and evaluated their antiproliferative activity by the MTT assay. The results displayed that, the hybrids of glycyrrhetinic acid ( 7a – 7b to 10a – 10b ) exhibited slightly better antiproliferative activity than that of ursolic acid hybrids ( 3a – 3b to 6a – 6b ). Two single glycyrrhetinic acid-thymine hybrids ( 8a and 10a ) possessed good antiproliferative activity against tested A549 cell line (IC 50  = 10.7 and 18.3 µM, respectively). And three hybrids ( 3a , 5a , and 10b ) exhibited about 80% inhibitory ratio against tested Hela cell line.