Cancer is a multifactorial disease and the second leading cause of death worldwide. Diverse factors induce carcinogenesis, such as diet, smoking, radiation, and genetic defects. The phosphatidylinositol 3-kinase (PI3Kα) has emerged as an attractive target for anticancer drug design. Eighteen derivatives of N-phenyl-6-chloro-4-hydroxy-2-quinolone-3-carboxamide were synthesized and characterized using FT-IR, NMR (1H and 13C), and high-resolution mass spectra (HRMS). The series exhibited distinct antiproliferative activity (IC50 µM) against human epithelial colorectal adenocarcinoma (Caco-2) and colon carcinoma (HCT-116) cell lines, respectively: compounds 16 (37.4, 8.9 µM), 18 (50.9, 3.3 µM), 19 (17.0, 5.3 µM), and 21 (18.9, 4.9 µM). The induced-fit docking (IFD) studies against PI3Kαs showed that the derivatives occupy the PI3Kα binding site and engage with key binding residues.

中文翻译：

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N-Phenyl-6-Chloro-4-Hydroxy-2-Quinolone-3-CarboxAmides：作为抗癌剂的分子对接、合成和生物学研究

癌症是一种多因素疾病，是全球第二大死亡原因。多种因素会诱发致癌作用，例如饮食、吸烟、辐射和遗传缺陷。磷脂酰肌醇 3-激酶 (PI3Kα) 已成为抗癌药物设计的一个有吸引力的目标。合成了 N-苯基-6-氯-4-羟基-2-喹诺酮-3-甲酰胺的 18 种衍生物，并使用 FT-IR、NMR（1H 和 13C）和高分辨率质谱 (HRMS) 对其进行了表征。该系列分别对人上皮结直肠腺癌 (Caco-2) 和结肠癌 (HCT-116) 细胞系表现出明显的抗增殖活性 (IC50 µM)：化合物 16 (37.4, 8.9 µM)、18 (50.9, 3.3 µM)、 19 (17.0, 5.3 µM) 和 21 (18.9, 4.9 µM)。