MetadataShow full item record
© 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.
Showing items related by title, author, creator and subject.
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 ...
Synthesis, biological evaluation and in silico and in vitro mode-of-action analysis of novel dihydropyrimidones targeting PPAR-yBharathkumar, H.; Paricharak, S.; Dinesh, K.; Siveen, S.; Fuchs, J.; Rangappa, S.; Mohan, C.; Mohandas, N.; Kumar, Alan Prem; Sethi, G.; Bender, A.; Basappa; Rangappa, K. (2014)Hepatocellular carcinoma, a fatal liver cancer, affects 600 000 people annually and ranks third in cancer-related lethality. In this work we report the synthesis and related biological activity of novel dihydropyrimidones. ...
Dolzhenko, Anton; Dolzhenko, A.; Chui, W. (2007)The substitution of hydrogen by fluorine as bioisosteric replacement has been practised widely in agricultural and medicinal chemistry. This has led to the discovery of many pesticides and therapeutically useful chemical ...