- Method for synthesizing 2-guanidinothiazole compound by one-pot process
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According to the invention, a substituted methyl ketone compound is innovatively used as a raw material, amidinothiourea is added into an alcohol solvent under the conditions of halogeno salt MX and Oxone, and a one-pot process one-step reaction is carried out to obtain the target 2-guanidinothiazole compound. Common methyl ketone is used for replacing an alpha-halogenated carbonyl compound whichis high in price and toxicity, MX which is low in price and easy to obtain is used as a halogen source, the method is novel, raw materials and reagents are cheap, reaction conditions are mild, and operation is easy and convenient, therefore low-cost, convenient and rapid synthesis of the 2-guanidinothiazole compound is achieved.
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Paragraph 0014
(2020/11/09)
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- Synthesis and biological evaluation of 2-amino-1-thiazolyl imidazoles as orally active anticancer agents
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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.
- 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
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scheme or table
p. 164 - 175
(2012/06/01)
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- Imidazolamino compounds
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The invention relates to novel imidazolamino compounds. Also disclosed are methods of treating cancer by using one of these compounds and pharmaceutical compositions containing one of these compounds.
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