Cancer, a noncommunicable disease, is the leading cause of mortality worldwide and is anticipated to rise by 75% in the next two decades, reaching approximately 25 million cases. Traditional cancer treatments, such as radiotherapy and surgery, have shown limited success in reducing cancer incidence. As a result, the focus of cancer chemotherapy has switched to the development of novel small molecule antitumor agents as an alternate strategy for combating and managing cancer rates. Heterocyclic compounds are such agents that bind to specific residues in target proteins, inhibiting their function and potentially providing cancer treatment. This review focuses on privileged heterocyclic pharmacophores with potent activity against carbonic anhydrases and kinases, which are important anticancer targets. Evaluation of ongoing pre-clinical and clinical research of heterocyclic compounds with potential therapeutic value against a variety of malignancies as well as the provision of a concise summary of the role of heterocyclic scaffolds in various chemotherapy protocols have also been discussed. The main objective of the article is to highlight key heterocyclic scaffolds involved in recent anticancer drug design that demands further attention from the drug development community to find more effective and safer targeted small-molecule anticancer agents.

癌症是一种非传染性疾病，是全世界死亡的主要原因，预计在未来二十年中将增加 75%，达到约 2500 万例。传统的癌症治疗方法，例如放射疗法和手术，在降低癌症发病率方面取得的成功有限。因此，癌症化疗的重点已转向开发新型小分子抗肿瘤药物，作为对抗和控制癌症发病率的替代策略。杂环化合物是与靶蛋白中的特定残基结合、抑制其功能并可能提供癌症治疗的试剂。本综述重点关注对碳酸酐酶和激酶（重要的抗癌靶标）具有有效活性的特殊杂环药效团。还讨论了对正在进行的对多种恶性肿瘤具有潜在治疗价值的杂环化合物的临床前和临床研究的评估，以及对杂环支架在各种化疗方案中的作用的简明总结。本文的主要目的是强调最近抗癌药物设计中涉及的关键杂环支架，这些支架需要药物开发界的进一步关注，以找到更有效、更安全的靶向小分子抗癌药物。