Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University. Riyadh 11451, Saudi Arabia.
Eur J Med Chem. 2010 Sep;45(9):4188-98. doi: 10.1016/j.ejmech.2010.06.013. Epub 2010 Jun 16.
Novel derivatives of quinazoline (1-27) have been synthesized and tested for their antitumor activity against three tumor cell lines among these cell lines the human breast carcinoma cell line (MCF-7) in which EGFR is highly expressed. All tested compounds showed potent and selective activity against breast cancer (MCF-7) with IC(50) range of 3.35-6.81 microg/ml. With regarding broad-spectrum activity compounds 5, 9, 15, 18 and 20 exploited potent antitumor against human liver cell line (HEPG2), human breast cell line (MCF-7) and human cervix cell line (HELA) with IC(50) range of 3.35-5.59 microg/ml. Virtual screening was carried out through docking the designed compounds into the ATP binding site of epidermal growth factor receptor (EGFR) to predict if these compounds have analogous binding mode to the EGFR inhibitors.
已经合成了喹唑啉（1-27）的新衍生物，并对其针对三种肿瘤细胞系的抗肿瘤活性进行了测试，其中包括人乳腺癌细胞系（MCF-7），其中 EGFR 高度表达。所有测试的化合物对乳腺癌（MCF-7）均表现出强大且选择性的活性，IC（50）范围为 3.35-6.81μg/ml。鉴于广谱活性，化合物 5、9、15、18 和 20 对人肝癌细胞系（HEPG2）、人乳腺癌细胞系（MCF-7）和人宫颈癌细胞系（HELA）表现出强大的抗肿瘤活性，IC（50）范围为 3.35-5.59μg/ml。通过将设计的化合物对接进入表皮生长因子受体（EGFR）的 ATP 结合位点进行虚拟筛选，以预测这些化合物是否具有与 EGFR 抑制剂类似的结合模式。
