期刊
INVESTIGATIONAL NEW DRUGS
卷 30, 期 1, 页码 164-175出版社
SPRINGER
DOI: 10.1007/s10637-010-9547-7
关键词
Microtubule; Cell cycle arrest; Apoptosis; Cytotoxicity; Orally active cancer therapeutics; Leukemia
资金
- National Health Research Institutes, Zhunan, Miaoli, Taiwan, R.O.C. [BP-090-PP01, BP-090-CF03, BP-091-CF03]
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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