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  • Title: Synthesis and biological evaluation of 2-amino-1-thiazolyl imidazoles as orally active anticancer agents.
    Author: Li WT, Hwang DR, Song JS, Chen CP, Chen TW, Lin CH, Chuu JJ, Lien TW, Hsu TA, Huang CL, Tseng HY, Lin CC, Lin HL, Chang CM, Chao YS, Chen CT.
    Journal: Invest New Drugs; 2012 Feb; 30(1):164-75. PubMed ID: 20890633.
    Abstract:
    Designed from a high throughput screened hit compound, novel 2-amino-1-thiazolyl imidazoles were synthesized and demonstrated cytotoxicity against human cancer cells. 1-(4-Phenylthiazol-2-yl)-4-(thiophen-2-yl)-1H-imidazol-2-amine (compound 2), a 2-amino-1-thiazolyl imidazole, inhibited tubulin polymerization, interacted with the colchicine-binding sites of tubulins, and caused cell cycle arrest at the G(2)/M phase in human gastric cancer cells. Disruption of the microtubule structure in cancer cells by compound 2 was also observed. Compound 2 concentration-dependently inhibited the proliferation of cancer cells in histocultured human gastric and colorectal tumors. Given orally, compound 2 prolonged the lifespans of leukemia mice intraperitoneally inoculated with the murine P388 leukemic cells. We report 2-amino-1-thiazolyl imidazoles as a novel class of orally active microtubule-destabilizing anticancer agents.
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