736176-76-4Relevant academic research and scientific papers
Synthesis and biological evaluation of 2-amino-1-thiazolyl imidazoles as orally active anticancer agents
Li, Wen-Tai,Hwang, Der-Ren,Song, Jen-Shin,Chen, Ching-Ping,Chen, Tung-Wei,Lin, Chi-Hung,Chuu, Jiunn-Jye,Lien, Tzu-Wen,Hsu, Tsu-An,Huang, Chen-Lung,Tseng, Huan-Yi,Lin, Chu-Chung,Lin, Heng-Liang,Chang, Chung-Ming,Chao, Yu-Sheng,Chen, Chiung-Tong
scheme or table, p. 164 - 175 (2012/06/01)
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)- 1Himidazol- 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 G2/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 microtubuledestabilizing anticancer agents. Springer Science+Business Media, LLC 2010.
