Alexander Rikki, Balasundaram Ahrani, Batchelor Mark, Brookings Daniel, Crépy Karen, Crabbe Tom, Deltent Marie-France, Driessens Frank, Gill Andrew, Harris Sue, Hutchinson Gillian, Kulisa Claire, Merriman Mark, Mistry Prakash, Parton Ted, Turner James, Whitcombe Ian, Wright Sara
Department of Medicinal Chemistry, UCB, 208 Bath Road, Slough, Berkshire SL1 3WE, UK.
Bioorg Med Chem Lett. 2008 Aug 1;18(15):4316-20. doi: 10.1016/j.bmcl.2008.06.076. Epub 2008 Jun 28.
4-(1,3-Thiazol-2-yl)morpholine derivatives have been identified as potent and selective inhibitors of phosphoinositide 3-kinase. The SAR data of selected examples are presented and the in vivo profiling of compound 18 is shown to demonstrate the utility of this class of compounds in xenograft models of tumor growth.
4-(1,3-噻唑-2-基)吗啉衍生物已被鉴定为磷酸肌醇3-激酶的强效和选择性抑制剂。本文给出了所选示例的构效关系数据,并展示了化合物18的体内分析结果,以证明这类化合物在肿瘤生长异种移植模型中的效用。