Synthesis and Molecular Docking Study of New Thiazole Derivatives as Potential Tubulin Polymerization Inhibitors.

ABSTRACT: A new series of 2,4-disubstituted thiazole derivatives containing 4-(3,4,5-trimethoxyphenyl) moiety was synthesized and evaluated for their potential anticancer activity as tubulin polymerization inhibitors. All designed compounds were screened for cytotoxic activity against four human cancer cell lines, namely, HepG2, MCF-7, HCT116, and HeLa, using 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide assay, with combretastatin A-4 as a reference drug. Compounds 5c, 6d, 7c, 8, and 9a,b showed superior activity against the tested cell lines, with IC₅₀ values ranging from 3.35 ± 0.2 to 18.69 ± 0.9 μM. Further investigation for the most active cytotoxic agents as tubulin polymerization inhibitors was also performed in ord

SUBMITTER: El-Abd AO 

PROVIDER: S-EPMC9494671 | biostudies-literature | 2022 Sep

REPOSITORIES: biostudies-literature