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© 2017 by the authors. Licensee MDPI, Basel, Switzerland. Exploring the pharmacologically important pyrazolo[1,5-a][1,3,5] triazin-7(6H)-one scaffold for the construction of new bioactive compounds, we developed a synthesis of 4-phenethylthio-2- phenylpyrazolo[1,5-a][1,3,5] triazin-7(6H)-one (4) via S-alkylation of 2-phenyl-4-thioxopyrazolo [1,5-a][1,3,5] triazine-7(6H)-one (3), prepared by the double ring closure of pyrazole and triazine rings upon the treatment of 1-cyanoacetyl-4-benzoylthiosemicarbazide (2) with alkali. The antiproliferative activity of 4 against human lung cancer (A549) and human breast cancer (MDA-MB231) cell lines was investigated. Compound 4 was found to be more active against lung cancer cells t han breast cancer cells.
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Synthesis and biological activity of fluorinated 7-aryl-2-pyridyl-6,7-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-5-amines.Dolzhenko, Anton; Tan, B.; Dolzhenko, A.; Chiu, G.; Chui, W. (2008)In our lead finding program, 12 new fluorinated 7-aryl-2-pyridyl-6,7-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-5-amines were prepared via a practical three-step procedure starting from (iso)nicotinic hydrazides. The ...
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