Concise synthesis and preliminary biological evaluation of new triazolylthioacetone derivatives bearing pyridine, pyrazine, and 3,4,5-trimethoxybenzyl fragment
Bioorganic & Medicinal Chemistry Letters（2022）
Abstract
•Based on our previous work, a series of triazolylthioacetones were synthesized.•IIc showed comparable potency with CA-4 on HT-29, HCT116, and HepG2 cells.•IIc exhibited the most potent antiproliferative activity on HT-29 with an IC50 of 0.62 μM.•IIc displayed a significant inhibition of tubulin polymerization with an IC50 value of 12.7 μM.
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Key words
Triazolylthioacetone,Synthesis,Tubulin polymerization inhibitor,Antiproliferative activity
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