Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 49, Issue 19, Pages 5769-5776Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm060545p
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Synthesis and cytotoxic activity in the submicromolar range of a series of [4-(imidazol-l-yl)thiazol-2-yl]-phenylamines are described. Cell cycle dependent cytotoxicity on RKO human colon carcinoma cells with inducible expression of p27(kip1) and the influence on microtubule formation were investigated. Considering the significant correlation between the IC50 values of tubulin polymerization inhibition, [H-3]colchicine competition, and cytotoxicity of the investigated compounds, tubulin is the main cellular target. The inhibition of microtubule formation was shown to be mediated by interference with the colchicine binding site of tubulin. In depth analysis of the investigated compounds allowed the identification of modifications that altered the pharmacological profile of the compounds from a mitosis-inducing phenotype to a G1 cell cycle arresting phenotype.
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