The development of drug resistance and severe side-effects has reduced the clinical efficacy of the existing anti-cancer drugs available in the market. Thus, there is always a constant need to develop newer anti-cancer drugs with minimal adverse effects. Researchers all over the world have been focusing on various alternative strategies to discover novel, potent, and target specific molecules for cancer therapy. In this direction, several heterocyclic compounds are being explored but amongst them one promising heterocycle is acridone which has attracted the attention of medicinal chemists and gained huge biological importance as acridones are found to act on different therapeutically proven molecular targets, overcome ABC transporters mediated drug resistance and DNA intercalation in cancer cells. Some of these acridone derivatives have reached clinical studies as these heterocycles have shown huge potential in cancer therapeutics and imaging. Here, the authors have attempted to compile and make some recommendations of acridone based derivatives concerning their cancer biological targets and in vitro-cytotoxicity based on drug design and novelty to increase their therapeutic potential. This review also provides some important insights on the design, receptor targeting and future directions for the development of acridones as possible clinically effective anti-cancer agents.

耐药性和严重副作用的发展降低了市场上现有抗癌药物的临床疗效。因此，始终需要开发副作用最小的新型抗癌药物。世界各地的研究人员一直在关注各种替代策略，以发现用于癌症治疗的新型、有效和靶向特定分子。在这个方向上，正在探索几种杂环化合物，但其中一种有前途的杂环是吖啶酮，它引起了药物化学家的注意并获得了巨大的生物学重要性，因为吖啶酮被发现可作用于不同的经治疗证明的分子靶点，克服 ABC 转运蛋白介导的耐药性和癌细胞中的DNA嵌入。这些吖啶酮衍生物中的一些已经进入临床研究，因为这些杂环在癌症治疗和成像方面显示出巨大的潜力。在这里，作者试图就吖啶酮衍生物的癌症生物学靶标和基于药物设计和新颖性的体外细胞毒性，以增加其治疗潜力。这篇综述还提供了一些关于吖啶酮作为可能的临床有效抗癌剂的设计、受体靶向和未来方向的重要见解。