Discovery and optimization of 3,4,5-trimethoxyphenyl substituted triazolylthioacetamides as potent tubulin polymerization inhibitors.
Bioorganic & Medicinal Chemistry Letters(2019)
摘要
•Based on our previous work, 29 novel triazolylthioacetamides possessing 3,4,5-trimethoxylphenyl groups were synthesized.•8f and 8j showed potent antiproliferative activities against Hela with IC50 values of 0.04 and 0.05 μM, respectively.•8b exhibited potent antitubulin activity with IC50 values of 5.9 μM, which was proximate to CA-4 (IC50 = 4.2 μM).
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关键词
Triazolylthioacetamides,Synthesis,Tubulin polymerization,Antiproliferative activity
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