Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P. O. Box 2457, Riyadh 11451, Saudi Arabia.
Molecules. 2013 Jan 24;18(2):1434-46. doi: 10.3390/molecules18021434.
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.
先前已经合成了一系列的 25 种 2-甲硫基-[1,2,4]三唑并[1,5-a]喹唑啉衍生物 1-25。现在，我们已经研究了它们对肝癌 Hep-G2 和结肠 HCT-116 癌细胞的细胞毒性作用，以及对巨噬细胞生长的影响，此外还研究了它们对炎症介质[一氧化氮（NO）、肿瘤坏死因子-α（TNF-α）、前列腺素 E-2（PGE-2）和细菌脂多糖（LPS）刺激的巨噬细胞]的影响。结果表明，化合物 13 和 17 表现出最高的细胞毒性，而化合物 3、6-8 和 25 是很有前途的多效抗炎剂。
