Waterson Alex G, Stevens Kirk L, Reno Michael J, Zhang Yue-Mei, Boros Eric E, Bouvier Frederic, Rastagar Abdullah, Uehling David E, Dickerson Scott H, Reep Bryan, McDonald Octerloney B, Wood Edgar R, Rusnak David W, Alligood Krystal J, Rudolph Sharon K
GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709-3398, USA.
Bioorg Med Chem Lett. 2006 May 1;16(9):2419-22. doi: 10.1016/j.bmcl.2006.01.111. Epub 2006 Feb 17.
Anilinoalkynylpyrimidines were prepared and evaluated as dual EGFR/ErbB2 kinase inhibitors. A preference was found for substituted phenyl and heteroaromatic rings attached to the alkyne. In addition, the presence of a potential hydrogen bond donor appended to this ring was favored. Selected molecules in the series demonstrated some activity against human tumor cell lines.
制备了苯胺基炔基嘧啶并将其作为双表皮生长因子受体（EGFR）/ 表皮生长因子受体2（ErbB2）激酶抑制剂进行评估。研究发现，连接在炔烃上的取代苯基和杂芳环更受青睐。此外，该环上连接潜在氢键供体的情况更有利。该系列中的部分分子对人类肿瘤细胞系表现出一定活性。
