Department of Pharmaceutical Chemistry, College of Pharmacy, Salman Bin Abdulaziz University, PO Box 173, Alkharj 11942, Saudi Arabia.
Eur J Med Chem. 2012 Jul;53:133-40. doi: 10.1016/j.ejmech.2012.03.044. Epub 2012 Apr 5.
A new series of substituted quinazolin-4-(3H)-one-tyrphostin derivatives was prepared and screened for their cytotoxic activity against three tumor cell lines, namely human breast cancer cell line (MCF-7), human cervical cancer cell line (HeLa) and human hepatocellular liver carcinoma cell line (HepG2) using the colorimetric MTT assay. Among the current series, 10 compounds exhibited remarkable in vitro antiproliferative activity against the three tested cell lines with the IC(50) values ranging from 0.009 to 0.015 mM. All the compounds showed suitable drug like characteristics according to Lipinski's rule.
我们合成了一系列新型取代喹唑啉-4(3H)-酮 tyrphostin 衍生物，并采用 MTT 比色法检测它们对三种肿瘤细胞系（人乳腺癌细胞系 MCF-7、人宫颈癌细胞系 HeLa 和人肝癌细胞系 HepG2）的细胞毒性。在所研究的化合物中，有 10 种化合物对三种测试细胞系表现出显著的体外抗增殖活性，IC50 值范围为 0.009 至 0.015mM。根据 Lipinski 规则，所有化合物均显示出适宜的类药性。
