412923-44-5Relevant articles and documents
Synthesis, SAR study, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase (FAAH) inhibitors
Kono, Mitsunori,Matsumoto, Takahiro,Kawamura, Toru,Nishimura, Atsushi,Kiyota, Yoshihiro,Oki, Hideyuki,Miyazaki, Junichi,Igaki, Shigeru,Behnke, Craig A.,Shimojo, Masato,Kori, Masakuni
, p. 28 - 41 (2013/02/22)
A series of piperazine ureas was designed, synthesized, and evaluated for their potential as novel orally available fatty acid amide hydrolase (FAAH) inhibitors that are therapeutically effective against pain. We carried out an optimization study of the l
One-pot tandem copper-catalyzed library synthesis of 1-thiazolyl-1,2,3- triazoles as anticancer agents
Li, Wen-Tai,Wu, Wan-Hsun,Tang, Chien-Hsiang,Tai, Ready,Chen, Shui-Tein
scheme or table, p. 72 - 78 (2011/04/17)
One-pot multicomponent synthesis to assemble compounds has been an efficient method for constructing a compound library. We have developed one-pot tandem copper-catalyzed azidation and CuAAC reactions that afford 1-thiazolyl-1,2,3-triazoles with anticancer activity. By utilizing this one-pot synthetic strategy, we constructed a library of 1-thiazolyl-1,2,3-triazoles in search of the potent lead compound. Furthermore, 1-thiazolyl-1,2,3-triazoles were evaluated for anticancer activity against the multidrug-resistant cancer cells MES-SA/Dx5. Most of the 1-thiazolyl-1,2,3-triazoles revealed cytotoxic effect against cancer cells at micromolar to low micromolar range. Testing some of the most potent compounds (5{4,2-4} and 5{5,1-3}) against the normal cell line Vero showed no significant toxicity (except 5{4,2}) to normal cells. This result indicates that compounds 5{4,3-4} and 5{5,1-3} possessed good potency and selectivity to cancer cells over normal cells.