Cytotoxic and Anti-Inflammatory Active Methylsulfanyltriazoloquinazolines

ISSN: 0973-7510

E-ISSN: 2581-690X

Rashad A. Al-Salahi¹ , Amira M. Gamal-Eldeen³, Amer M. Alanazi¹, Mohamed A. Al-Omar¹, Mohamed A. Marzouk^1,2 and Moustafa M.G. Fouda^4,5

¹Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P. O. Box 2457, Riyadh 11451, Saudi Arabia.

²Chemistry 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.

J Pure Appl Microbiol. 2013;7(Spl. Edn.: November):189-198

Received: 25/08/2013 | Accepted: 22/10/2013 | Published: 30/11/2013

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

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