Waterson Alex G, Petrov Kimberly G, Hornberger Keith R, Hubbard Robert D, Sammond Douglas M, Smith Stephon C, Dickson Hamilton D, Caferro Thomas R, Hinkle Kevin W, Stevens Kirk L, Dickerson Scott H, Rusnak David W, Spehar Glenn M, Wood Edgar R, Griffin Robert J, Uehling David E
GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709-3398, USA.
Bioorg Med Chem Lett. 2009 Mar 1;19(5):1332-6. doi: 10.1016/j.bmcl.2009.01.080. Epub 2009 Feb 7.
Aniline 'headgroups' were synthesized and incorporated into an alkynyl thienopyrimidine series of EGFR and ErbB-2 inhibitors. Potent inhibition of enzyme activity and cellular proliferation was observed. In certain instances, protein binding was reduced and oral exposure was found to be somewhat improved relative to compounds containing the reference aniline.
合成了苯胺“头基”并将其引入到一系列用于表皮生长因子受体（EGFR）和ErbB - 2抑制剂的炔基噻吩并嘧啶中。观察到对酶活性和细胞增殖有强效抑制作用。在某些情况下，与含有参考苯胺的化合物相比，蛋白质结合减少，口服暴露有所改善。
