Sixteen new 2-substituted quinazolines were synthesized using a straightforward methodology starting from 2-methoxybezoic acid or 3-methoxy-2-naphthoic acid. The anti-proliferative activity of the target compounds was evaluated against nine cancer cell lines. Additionally, all the compounds were screened for their potency and selectivity against a panel of 109 kinases and four bromodomains, using Differential Scanning Fluorimetry (DSF). Compound 17 bearing a 2-methoxyphenyl substitution along with a basic side chain displayed a remarkable profile against the majority of the tested cell lines.

中文翻译：

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具有抗增殖活性的2-取代喹唑啉-4(3H)-的合成及生物学评价


以 2-甲氧基苯甲酸或 3-甲氧基-2-萘甲酸为原料，采用简单的方法合成了 16 种新的 2-取代喹唑啉。针对九种癌细胞系评估了目标化合物的抗增殖活性。此外，还使用差示扫描荧光测定法 (DSF) 筛选了所有化合物针对一组 109 种激酶和四种溴结构域的效力和选择性。带有 2-甲氧基苯基取代以及碱性侧链的化合物 17 对大多数测试的细胞系表现出显着的特征。