Department of Pharmacognosy, Perm State Pharmaceutical Academy, 2 Polevaya Street, 614081 Perm, Russia
Ekaterina V. Gorgopina
Department of General and Organic Chemistry, Perm State Pharmaceutical Academy, 2 Polevaya Street, 614081 Perm, Russia
Vera R. Lezhnyova
Department of General and Organic Chemistry, Perm State Pharmaceutical Academy, 2 Polevaya Street, 614081 Perm, Russia
Gwyneth En-Tian Ong
Department of Pharmacy, Faculty of Science, National University of Singapore, 18 Science Drive 4, Singapore 117543, Singapore
Wai-Keung Chui
Department of Pharmacy, Faculty of Science, National University of Singapore, 18 Science Drive 4, Singapore 117543, Singapore
Anton V. Dolzhenko
School of Pharmacy, Curtin Health Innovation Research Institute, Faculty of Health Sciences, Curtin University, GPO Box U1987, Perth, Western Australia 6845, Australia
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 than breast cancer cells.
