Substituted 3-(5-Imidazo[2,1-b]thiazolylmethylene)-2-indolinones and Analogues: Synthesis, Cytotoxic Activity, and Study of the Mechanism of Action

Citations Over TimeTop 10% of 2012 papers

Abstract

The synthesis of substituted 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones and analogues is reported. Their cytotoxic activity was evaluated according to protocols available at the National Cancer Institute (NCI), Bethesda, MD. The action of selected compounds was examined for potential inhibition of tubulin assembly in comparison with the potent colchicine site agent combretastatin A-4. The most potent compounds also strongly and selectively inhibited the phosphorylation of the oncoprotein kinase Akt in cancer cells. The effect of the most interesting compounds was examined on the growth of HT-29 colon cancer cells. These compounds caused the cells to arrest in the G2/M phase of the cell cycle, as would be expected for inhibitors of tubulin assembly.

Related Papers

• → Interactions of colchicine with tubulin(1991)283 cited
• → β-III Tubulin Levels Determine the Neurotoxicity Induced by Colchicine-Site Binding Agent Indibulin(2022)10 cited
• → Biochemical determination of tubulin-microtubule equilibrium in cultured cells(1979)40 cited
• → B‐ring of colchicine and its role in taxol‐induced tubulin polymerization(1986)4 cited
• → A modified colchicine-binding assay for the measurement of total and microtubule-derived tubulin in rat liver(1983)15 cited