Synthesis of spin labeled Aurora A kinase inhibitors

• 作 者: Wen-WenQin;Shi-WuChen;
• 机 构: School of Pharmacy,Lanzhou University,Lanzhou 730000,P.R.China
• 出 处: 全国药物化学学术会议暨第四届中英药物化学学术会议
• 发表日期: 2013年期

　　Aurora kinases are a family of mitotic serine/threonine kinases,which have been implicated in several vital events in mitosis.[1]Deregulation of Aurora kinase activity can result in mitotic abnormality and genetic instability.So they have received significant attention as new targets for anticancer therapy.Recently,it was reported that a class of 2,4-bisanilinopyrimidine were Aurora A inhibitors with excellent selectively for Aurora A over Aurora B.However,their antiproliferative activities were not high due to their low solubility and/or permeability.The stable nitroxides are effective transporter and helping to increase the solubility of drugs.[2]In order to find effective antitumor drugs selectively targeted to Aruroa A kinase,two series of stable nitroxides labeled pyrimidines were designed,synthesized,and evaluated for their biological activities including enzyme assays,cellular assays,antitumor activities in vitro and in vivo,and their action mechanism.At present,we have obtained several compounds and their biological activities are being tested.This course will provide a promising direction to find new targeting antitumor drugs.