单羧酸转运蛋白（MCTs）由于在肿瘤代谢中扮演着至关重要的角色，已经引起了癌症研究的广泛关注。MCTs作为一种在癌细胞中转运乳酸分子的传奇，是糖酵解的产物和废物，作为肿瘤增殖的不可或缺因素。利用抑制剂靶向MCTs已经成为一种有前景的抗癌策略。本文总结了关于MCT抑制剂在预防癌症发生中的最新研究，涵盖了杂环和非杂环化合物。已有报道显示，如喋啶、吡唑、吲哚、类黄酮、香豆素衍生物和腈乙酸衍生物等杂环和非杂环化合物具有有效的MCT抑制作用。本文探讨了MCT在癌症代谢中的分子基础，杂环和非杂环MCT抑制剂的设计和合成，它们对肿瘤细胞和微环境的影响以及作为治疗药物的潜力。此外，我们探讨了MCT抑制剂开发所面临的挑战，并提出了推动该领域发展的未来方向。这篇写作旨在为研究人员、科学家和临床医生提供关于杂环和非杂环MCT抑制剂及其在抗癌中的潜力的全面理解。© 2023 John Wiley & Sons Ltd.

Monocarboxylate transporters (MCTs) have gained significant attention in cancer research due to their critical role in tumour metabolism. MCTs are legends for transporting lactate molecules in cancer cells, an oncometabolite and waste product of glycolysis, acting as an indispensable factor of tumour proliferation. Targeting MCTs with inhibitors has emerged as a promising strategy to combat tumorigenesis. This article summarizes the most recent research on MCT inhibitors in preventing carcinogenesis, covering both heterocyclic and non-heterocyclic compounds. Heterocyclic and non-heterocyclic compounds such as pteridine, pyrazole, indole, flavonoids, coumarin derivatives and cyanoacetic acid derivatives have been reported as potent MCT inhibitors. We examine the molecular underpinnings of MCTs in cancer metabolism, the design and synthesis of heterocyclic and non-heterocyclic MCT inhibitors, their impact on tumour cells and the microenvironment and their potential as therapeutic agents. Moreover, we explore the challenges associated with MCT inhibitor development and propose future directions for advancing this field. This write-up aims to provide researchers, scientists and clinicians with a comprehensive understanding of the heterocyclic and non-heterocyclic MCT inhibitors and their potential in combating tumorigenesis.© 2023 John Wiley & Sons Ltd.