Abstract：
Quinolone is a heterocyclic compound containing carbonyl at the C-2 or C-4 positions with nitrogen at the C-1 position. The scaffold was first identified for its antibacterial properties, and the derivatives were known to possess many pharmacological activities, including anticancer. In this review, the quinolin-2(H)-one and quinolin-4(H)-one derivatives were identified to inhibit several various proteins and enzymes involved in cancer cell growth, such as topoisomerase, mi-crotubules, protein kinases, phosphoinositide 3-kinases (PI3K) and histone deacetylase (HDAC). Hybrids of quinolone with curcumin or chalcone, 2-phenylpyrroloquinolin-4-one and 4-quinolone derivatives have demonstrated strong potency against cancer cell lines. Additionally, quinolones have been explored as inhibitors of protein kinases, including EGFR and VEGFR. Therefore, this review aims to consolidate the medicinal chemistry of quinolone derivatives in the pipeline and discuss their similarities in terms of their pharmacokinetic profiles and potential target sites to provide an understanding of the structural requirements of anticancer quinolones.
摘要：
喹诺酮是在C-2或C-4位含有羰基且在C-1位含有氮的杂环化合物。该支架首先被确定为其抗菌性能，已知这些衍生物具有许多药理活性，包括抗癌。在这次审查中,喹啉-2（H）-酮和喹啉-4（H）-酮衍生物被鉴定为抑制参与癌细胞生长的几种不同的蛋白质和酶，如拓扑异构酶，微管，蛋白激酶，磷酸肌醇3-激酶（PI3K）和组蛋白脱乙酰酶（HDAC）。喹诺酮与姜黄素或查尔酮的杂种，2-苯基吡咯并喹啉-4-酮和4-喹诺酮衍生物已证明对癌细胞系的强效力。此外,喹诺酮类药物已被用作蛋白激酶的抑制剂，包括EGFR和VEGFR。因此,这篇综述旨在巩固喹诺酮衍生物的药物化学，并讨论它们在药代动力学特征和潜在靶位点方面的相似性，以了解抗癌喹诺酮类的结构要求。
