期刊
BIOORGANIC CHEMISTRY
卷 104, 期 -, 页码 -出版社
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2020.103909
关键词
1,2,4-triazole; Antiproliferative activity; Colchicine binding site inhibitor; Molecular docking
资金
- National Natural Science Foundation of China [81673293, 81602969]
- China Postdoctoral Science Foundation [2018M641715]
- Liaoning Revitalization Talents Program [XLYC1802072]
- Plan for Development of Young Scholars of Shenyang pharmaceutical university [ZQN2018002]
- Program for Innovative Research Team of the Ministry of Education
A series of novel 5-methyl-4-aryl-3-(4-arylpiperazine-1-carbonyl)-4H-1,2,4-triazoles possessing 1,2,4-triazole as the hydrogen-bond acceptor were designed, synthesized and evaluated for their antiproliferative and tubulin polymerization inhibitory activities. Some of them exhibited moderate activities in vitro against the three cancer cell lines including SGC-7901, A549 and HeLa. Compound 6e exhibited the highest potency against the three cancer cell lines. Moreover, the tubulin polymerization experiments indicated that compound 6e could inhibit the tubulin polymerization. Immunofluorescence study and cell cycle analysis clearly revealed compound 6e could disrupt intracellular microtubule organization, arrest cell cycle at the G2/M phase. In addition, molecular docking analysis demonstrated the interaction of compound 6e at the colchicine-binding site of tubulin. These preliminary results suggested that compound 6e is a new colchicine binding site inhibitor and worthy of further investigation.
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