A series of 5,7-disubstituted quinazolines, bearing 4-heteroaryl substituents such as 2-pyridinylamine or 2-pyrazinylamine, has been synthetised and evaluated as c-Src kinase inhibitors. Highly potent inhibition, high selectivity and physical properties suitable for oral dosing were achieved within this series: 23d and 42 were identified as sub-0.1muM inhibitors in a c-Src-driven cell proliferation assay and displayed adequate rat pharmacokinetics after oral administration.

中文翻译：

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作为有效的和选择性的c-Src激酶抑制剂的4-（2-氯-5-甲氧基苯胺基）喹唑啉的新杂环类似物。

已合成了一系列带有4-杂芳基取代基（如2-吡啶基胺或2-吡嗪基胺）的5,7-二取代喹唑啉，并将其评估为c-Src激酶抑制剂。在该系列中实现了适用于口服给药的高效抑制作用，高选择性和物理特性：在c-Src驱动的细胞增殖测定中，23d和42被鉴定为亚0.1μM抑制剂，并在口服后显示出足够的大鼠药代动力学。