Li, Wen-TaiWen-TaiLiWu, Wan-HsunWan-HsunWuTang, Chien-HsiangChien-HsiangTangTai, ReadyReadyTaiChen, Shui-TeinShui-TeinChen2012-10-202018-07-062012-10-202018-07-062011http://ntur.lib.ntu.edu.tw//handle/246246/243401One-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. ? 2010 American Chemical Society.en-US1-thiazolyl-1,2,3-triazole; CuAAC reaction; Cytotoxic activity; One-pot synthesis[SDGs]SDG3antineoplastic agent; copper; triazole derivative; article; catalysis; chemistry; fluorescence; scanning electron microscopy; synthesis; Antineoplastic Agents; Catalysis; Copper; Fluorescence; Microscopy, Electron, Scanning; Triazolesjournal article10.1021/co1000234http://ntur.lib.ntu.edu.tw/bitstream/246246/243401/-1/89.pdf