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• Al-Salahi, RA.
• Gamal-Eldeen, AM.
• Alanazi, AM.
• Al-Omar, MA.
• Marzouk, MA.
• Fouda, MM. G.
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• Al-Salahi, RA.
• Gamal-Eldeen, AM.
• Alanazi, AM.
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• Fouda, MM. G.
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• Gamal-Eldeen, AM.
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Molecules 2013, 18(2), 1434-1446; doi:10.3390/molecules18021434

Article

Cytotoxicity and Anti-Inflammatory Activity of Methylsulfanyl-triazoloquinazolines

Rashad A. Al-Salahi ^1,* , Amira M. Gamal-Eldeen ² , Amer M. Alanazi ¹ , Mohamed A. Al-Omar ¹ , Mohamed A. Marzouk ^1,3  and Moustafa M. G. Fouda ^4,5

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

* Author to whom correspondence should be addressed.

Received: 24 December 2012; in revised form: 10 January 2013 / Accepted: 14 January 2013 / Published: 24 January 2013

Download PDF Full-Text [209 KB, uploaded 24 January 2013 13:26 CET]

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-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.

Keywords: 1,2,4-triazoloquinazoline; antitumor; Hep-G2; HCT-116; inflammation

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