Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, PO Box 2457, Riyadh 11451, Saudi Arabia.
Bioorg Med Chem Lett. 2012 Mar 1;22(5):1879-85. doi: 10.1016/j.bmcl.2012.01.071. Epub 2012 Jan 28.
A novel series of 7-substituted-4(3H)-quinazolinone were designed, synthesized and evaluated for their antitumor and anticonvulsant activity. Compound 7 revealed broad-spectrum antitumor effectiveness toward numerous cell lines that belong to different tumor subpanels, whereas compounds 9 and 18 possess selective activity toward leukemia cell lines. Additionally, compounds 3, 15, 16, 18, 19 and 20 showed advanced anticonvulsant activity as well as lower neurotoxicity than reference drugs. The achieved results proved that the distinctive compounds could be valuable as a model for future devise, acclimatization and investigation to construct more active analogues.
设计、合成了一系列 7-取代-4(3H)-喹唑啉酮，并对其抗肿瘤和抗惊厥活性进行了评价。化合物 7 对属于不同肿瘤亚类的多种细胞系表现出广谱抗肿瘤效果，而化合物 9 和 18 对白血病细胞系具有选择性活性。此外，化合物 3、15、16、18、19 和 20 表现出较强的抗惊厥活性和比参考药物更低的神经毒性。所得结果证明，这些独特的化合物可作为未来设计、适应和研究更具活性类似物的模型，具有重要价值。
