Abstract VEGFR-2 inhibition represents an attractive strategy for anticancer drug design. A new series of quinoline derivatives were synthesized and structurally confirmed with different spectroscopic techniques. VEGFR-2 inhibition assay showed that 2-(4-bromoquinolin-3-yloxy)-1-(4-chlorophenyl)ethanone ( V ) demonstrated potent VEGFR-2 inhibitory activities. In addition, the brominated quinoline ( V ) exhibit antitumor activity over MCF-7 cell line via cell cycle arrest at G1 phase and apoptosis inducing activity as revealed by cell cycle analysis and Annexin V/FITC staining assays. Moreover, brominated quinoline ( V ) was proved to upregulate expression of proteins that trigger apoptosis such as increased Bax, decreased Bcl-2 as well as increased Bax/Bcl-2 ratio.

中文翻译：

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基于 MCF-7 乳腺癌细胞系的新型喹啉衍生物的设计、合成和细胞毒性筛选

摘要 VEGFR-2 抑制代表了一种有吸引力的抗癌药物设计策略。合成了一系列新的喹啉衍生物，并用不同的光谱技术对其进行了结构确认。VEGFR-2 抑制试验表明 2-(4-bromoquinolin-3-yloxy)-1-(4-chlorophenyl)ethanone (V) 显示出有效的 VEGFR-2 抑制活性。此外，如细胞周期分析和膜联蛋白 V/FITC 染色分析所揭示的，溴化喹啉 (V) 通过在 G1 期的细胞周期停滞和诱导细胞凋亡的活性表现出对 MCF-7 细胞系的抗肿瘤活性。此外，溴化喹啉 (V) 被证明可以上调触发细胞凋亡的蛋白质的表达，例如 Bax 增加、Bcl-2 减少以及 Bax/Bcl-2 比率增加。