Zhejiang Betapharma, 589 Hongfong Rd., YuhangDistrict, Zhejiang 311100, PR China.
Bioorg Med Chem Lett. 2012 Oct 1;22(19):6301-5. doi: 10.1016/j.bmcl.2012.06.067. Epub 2012 Jun 28.
Crown ether fused anilinoquinazoline analogues were synthesized as novel epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors. Representative compounds showed potent and selective EGFR inhibitory activities in an in vitro EGFR kinase assay and an EGFR-mediated intracellular tyrosine phosphorylation assay. The synthesis and preliminary biological, physical, and pharmacokinetic evaluation of these fused quinazoline compounds is reported.
冠醚融合苯胺喹唑啉类似物被合成为新型表皮生长因子受体（EGFR）酪氨酸激酶抑制剂。代表性化合物在体外 EGFR 激酶测定和 EGFR 介导的细胞内酪氨酸磷酸化测定中表现出很强的选择性 EGFR 抑制活性。本文报道了这些融合喹唑啉类化合物的合成及初步的生物、物理和药代动力学评价。
