N6-methyladenosine (m6A) modification is a common form of RNA epigenetic regulation, playing crucial roles in various physiological processes and cancer development. Abnormal m6A expression in cancer tissues promotes tumor growth, metastasis, drug resistance, and immune evasion. This review comprehensively summarizes the classification and functions of m6A regulators, highlighting their interactions with key cancer pathways. It also provides an overview of small molecule inhibitors targeting m6A regulators, detailing their development, mechanism of action, pharmacology, and structure-activity relationships. The review aims to offer insights for future drug design and optimization, emphasizing the potential of m6A as a therapeutic target in cancer treatment. Key m6A regulators, such as METTL3, FTO, and YTHDF1, are discussed in detail, along with their roles in cancer proliferation, metastasis, drug resistance, and immune responses. The review highlights the therapeutic potential of targeting m6A regulators in cancer therapy, providing a comprehensive understanding of their complex mechanisms and their significance in anti-tumor strategies.N6-methyladenosine (m6A) modification is a common form of RNA epigenetic regulation, playing crucial roles in various physiological processes and cancer development. Abnormal m6A expression in cancer tissues promotes tumor growth, metastasis, drug resistance, and immune evasion. This review comprehensively summarizes the classification and functions of m6A regulators, highlighting their interactions with key cancer pathways. It also provides an overview of small molecule inhibitors targeting m6A regulators, detailing their development, mechanism of action, pharmacology, and structure-activity relationships. The review aims to offer insights for future drug design and optimization, emphasizing the potential of m6A as a therapeutic target in cancer treatment. Key m6A regulators, such as METTL3, FTO, and YTHDF1, are discussed in detail, along with their roles in cancer proliferation, metastasis, drug resistance, and immune responses. The review highlights the therapeutic potential of targeting m6A regulators in cancer therapy, providing a comprehensive understanding of their complex mechanisms and their significance in anti-tumor strategies.