Journal of Pure and Applied MicrobiologyVol. 7 No. Special Edition Nov. 2013

Cytotoxic and Anti-Inflammatory Active Methylsulfanyltriazoloquinazolines

Rashad A. Al-Salahi1*, Amira M. Gamal-Eldeen2, Amer M. Alanazi1, Mohamed A. Al-Omar1, Mohamed A. Marzouk1,3 and Moustafa M.G. Fouda4,5

1Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P. O. Box 2457, Riyadh 11451, Saudi Arabia. 2 Chemistry of Natural products Group, Center of Excellence for Advanced Sciences, National Research Center, Dokki 12622, Cairo, Egypt. 3Cancer Biology Group, Center of Excellence for Advanced Sciences, National Research Center, Dokki 12622, Cairo, Egypt. 4Petrochemical Research Chair, Chemistry Department, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia. 5Textile Research Division, National Research Center, Dokki 12622, Cairo, Egypt.

Received on 25 August 2013 and accepted on 22 October 2013

 

ABSTRACT

A series of twenty five 2-methylsulfanyl-[1,2,4]triazolo[1,5-a]quinazoline derivatives 1?25 was previously synthesized. We have now investigated their cytotoxic effects against hepatocellular Hep-G2 and colon HCT-116 carcinoma cells and effect on the macrophage growth, in addition to their influence of the inflammatory mediators [nitric oxide (NO), tumor necrosis factor-a (TNF-a), prostaglandin E-2 (PGE-2) and in bacterial lipopolysachharide (LPS)-stimulated macrophages]. The findings revealed that compounds 13 and 17 showed the highest cytotoxicity and that 3, 6?8 and 25 are promising multipotent anti-inflammatory agents.

Keywords : 1,2,4-Triazoloquinazoline; Antitumor; Hep-G2; HCT-116; Inflammation.