Acta Pharm. 67 (2017) 407-414
Pharmacological activities of some triazinopyrazolothieno pyrimidine derivatives
SALEH A. BAHASHWAN
Taibah University, Faculty of Pharmacy, Department of Pharmacology and Toxicology, Madinah Munawara, Saudi Arabia
Accepted April 14, 2017
Published online May 8, 2017
Triazinopyrazolothieno pyrimidine derivatives 1–5 were evaluated for their anti-inflammatory, analgesic and anticancer activities and acute toxicity. Anti-inflammatory activity of the compounds was studied using the carrageenan test. All tested compounds showed analgesic activity, 3-methoxycarbonyl-4,6-dimethyl-8-[(N-methylindolyl)methyl]pyrimido [5',4':4,5]thieno [3',2'-3,4]pyrazolo [5,1-c]triazine (4) showed activity comparable to that of diclofenac. Compounds 1–5 were also screened for anticancer activity on a human lung cancer cell line (A549) and a human prostate cancer cell line (DU145) using the MTT micro-cultured tetrazolium assay method. Compound 4 showed also significant anticancer activity against both cancer cell lines, comparable to that of doxorubicin. The most active compounds were tested for their acute toxicity and median lethal doses were evaluated.
Keywords: pyrimidine derivatives, triazinopyrazolothieno, anti-inflammatory, analgesic, anticancer, acute toxicity