喹诺酮骨架是一个带有氮在第一位置和一个羰基在第二或第四位置的双环苯-吡啶骨架。它具有多样的药理活性，包括抗肿瘤活性，并已进入临床试验的各种发展阶段，用于其特定靶向抗癌活性。本综述涵盖了喹诺酮类化合物的两个类别，即喹啉-2(H)-酮和喹啉-4(H)-酮，以及其可能的结合模式。此外，还对其结构-活性关系、分子机制和药代动力学性质进行了讨论，以便深入了解其抗癌药物的合理设计所需的结构要求。合成可行性和在多个位置易于衍生化的便利性，使药物化学家能够探索喹诺酮及其化学多样性，以发现更新的抗癌药物。基本骨架中同时存在氢键供体(-NH) 和受体(-C=O) 在两个不同的位置上的功能，拓宽了研究范围。特别是在喹诺酮基团的 -NH官能团上的取代，为合适的功能化和喹诺酮的第三、第六、第七个碳的适当取代提供了充足的空间，从而实现了与各种药物靶标特异性结合的选择性抗癌药物的发现。

The quinolone scaffold is a bicyclic benzene-pyridinic ring scaffold with nitrogen at the first position and a carbonyl group at the second or fourth position. It is endowed with a diverse spectrum of pharmacological activities, including antitumor activity, and has progressed into various development phases of clinical trials for their target-specific anticancer activity.The present review covers both classes of quinolones, i.e. quinolin-2(H)-one and quinolin-4(H)-one as anticancer agents, along with their possible mode of binding. Furthermore, their structure-activity relationships, molecular mechanisms, and pharmacokinetic properties are also covered to provide insight into their structural requirements for their rational design as anticancer agents.Synthetic feasibility and ease of derivatization at multiple positions, has allowed medicinal chemists to explore quinolones and their chemical diversity to discover newer anticancer agents. The presence of both hydrogen bond donor (-NH) and acceptor (-C=O) functionality in the basic scaffold at two different positions, has broadened the research scope. In particular, substitution at the -NH functionality of the quinolone motif has provided ample space for suitable functionalization and appropriate substitution at the quinolone's third, sixth, and seventh carbons, resulting in selective anticancer agents binding specifically with various drug targets.