合成及 4-苯胺基喹啉查尔酮衍生物的抗癌评价。
Synthesis and Anticancer Evaluation of 4-Anilinoquinolinylchalcone Derivatives.
机构信息
Department of Medicinal and Applied Chemistry, College of Life Science, Kaohsiung Medical University, Kaohsiung City 80708, Taiwan.
Graduate Institute of Medicine, College of Medicine, Kaohsiung Medical University, Kaohsiung 80708, Taiwan.
出版信息
Int J Mol Sci. 2023 Mar 23;24(7):6034. doi: 10.3390/ijms24076034.
A series of 4-anilinoquinolinylchalcone derivatives were synthesized and evaluated for antiproliferative activities against the growth of human cancer cell lines (Huh-7 and MDA-MB-231) and normal lung cells (MRC-5). The results exhibited low cytotoxicity against human lung cells (MRC-5). Among them, ()-3-{4-{[4-(benzyloxy)phenyl]amino}quinolin-2-yl}-1-(4-methoxyphenyl) prop-2-en-1-one () was found to have the highest cytotoxicity in breast cancer cells and low cytotoxicity in normal cells. Compound causes ATP depletion and apoptosis of breast cancer MDA-MB-231 cells and triggers reactive oxygen species (ROS)-dependent caspase 3/7 activation. In conclusion, it is worth studying 4-anilinoquinolinylchalcone derivatives further as new potential anticancer agents for the treatment of human cancers.
一系列 4-苯胺基喹啉基查耳酮衍生物被合成并评估了它们对人癌细胞系（Huh-7 和 MDA-MB-231）和正常肺细胞（MRC-5）生长的增殖活性。结果显示对人肺细胞（MRC-5）的细胞毒性低。其中，（）-3-{4-{[4-（苯甲氧基）苯基]氨基}喹啉-2-基}-1-（4-甲氧基苯基）-2-烯-1-酮（）在乳腺癌细胞中显示出最高的细胞毒性，而在正常细胞中细胞毒性低。化合物 导致乳腺癌 MDA-MB-231 细胞的 ATP 耗竭和凋亡，并引发活性氧（ROS）依赖性半胱天冬酶 3/7 激活。总之，作为治疗人类癌症的新型潜在抗癌药物，4-苯胺基喹啉基查耳酮衍生物值得进一步研究。
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