期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 75, 期 -, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2022.128978
关键词
[1,2,4]Triazolo[4,3-a]pyridine; Synthesis; Antiproliferative activity
资金
- Open Project of Guangdong Provincial Key Laboratory of New Drug Screening [GDKLNDS- 2021OF001]
- Special Funds for the Cultivation of Guangdong College Students' Scientific and Technological Innovation (Climbing Program Special Funds) [pdjh2020b0117]
- Natural Science Foundation of Guangdong Province, China [2018B030311067]
A novel series of 6-arylamino-[1,2,4]triazolo[4,3-a]pyridine derivatives were synthesized and evaluated for their antiproliferative activities. Inserting an amino linkage between the 6-aryl group and [1,2,4]triazolo[4,3-a]pyridine core resulted in a broader antitumor spectrum. Compound 8l exhibited potent and broad-spectrum antiproliferative activity, inducing cell cycle arrest and apoptosis. These findings suggest significant potential for the discovery of new highly efficient anticancer agents.
Based on our previous work, a series of novel 6-arylamino-[1,2,4]triazolo[4,3-a]pyridine derivatives were synthesized, and evaluated for antiproliferative activities. SAR studies revealed that inserting an amino linkage between 6-aryl group and [1,2,4]triazolo[4,3-a]pyridine core led to a much broader antitumor spectrum, and the most promising compound 8 l exerted potent and broad-spectrum antiproliferative activity toward HeLa, HCT116, MCF-7, and A549 cell lines, with IC50 values in the micromolar range of 5.98-12.58 mu M, which were more active than the positive control 5-FU. The mechanism investigation illustrated that 8 l dose-dependently caused cell cycle arrest at the G2/M phase, and induced cell apoptosis in HeLa cells. Consequently, these find-ings suggest the 6-arylamino-[1,2,4]triazolo[4,3-a]pyridines afford significant potential for the discovery of a new highly efficient anticancer agents.
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