Discovery of Lead Structures against Tumor Angiogenesis Based on VEGFR Tyrosin Kinase as Target

• 作 者: WenfangXu;FumingXu;LeiZhang;
• 机 构: Department of Medicinal Chemistry,School of Pharmaceutical Sciences,Shandong University,44 West Cult
• 出 处: 第九届IUPAC化学生物学国际研讨会暨第八届世界华人药物化学研讨会
• 发表日期: 2012年期

　　A virtual screening approach was performed to develop novel and potent vascularendothelial growth factor receptor 2(VEGFR2) inhibitors.A4-aminonaphthalen-1-ol group containing molecule SO1 showed good performance in the study.In the following tube formation assay using HUVECs1 and the rat thoracic aorta rings test2,SO1 was discovered to efficiently inhibit angiogenesis.A series of novel4-aminonaphthalen-1-ol derivatives were synthesized and screened for in vitro anticancer and antiangiogenesis activities.One of them,M09,exhibited much better antiangiogenic activity than S01 did.Further kinase assay3 study showed that compound M09 has good VEGFR2,ALK and ABL inhibitory activities.