Department of Chemistry, Korea Advanced Institute of Science and Technology, Daejeon, 305-701, Korea.
Org Lett. 2010 Mar 19;12(6):1212-5. doi: 10.1021/ol100011n.
An efficient and versatile synthetic approach for the preparation of highly substituted xanthine derivatives has been developed by a combination of direct N7- and C8-arylation. With this method, diverse xanthine analogues were prepared and potent kinase inhibitors could be identified. For example, compound 8a inhibits PI3Ks and proliferation in T47D tumor cells. In addition, these xanthine-based kinase inhibitors exhibited significant fluorescence emission in a concentration-dependent response.
已开发出一种高效、通用的合成方法，通过直接 N7-和 C8-芳基化组合制备高度取代的黄嘌呤衍生物。使用该方法，制备了多种黄嘌呤类似物，并鉴定出有效的激酶抑制剂。例如，化合物 8a 抑制 T47D 肿瘤细胞中的 PI3Ks 和增殖。此外，这些基于黄嘌呤的激酶抑制剂在浓度依赖性响应中表现出显著的荧光发射。
