Cytotoxicity and Anti-Inflammatory Activity of Methylsulfanyl-triazoloquinazolines

• Main Authors: Moustafa M. G. Fouda, Mohamed A. Marzouk, Mohamed A. Al-Omar, Amer M. Alanazi, Rashad A. Al-Salahi, Amira M. Gamal-Eldeen
• Format: Article
• Language: English
• Published: MDPI AG 2013-01-01
• Series: Molecules
• Subjects: 1,2,4-triazoloquinazoline; antitumor; Hep-G2; HCT-116; inflammation
• Online Access: http://www.mdpi.com/1420-3049/18/2/1434

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-α (TNF-α), 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 multi-potent anti-inflammatory agents.