DNA甲基转移酶（DNMT）是保守的一类胞嘧啉甲基酶家族，在表观遗传学调控中起着至关重要的作用。它们被认为是治疗癌症的有希望的靶点。在DNMT家族中，DNMT3A亚型的突变在血液恶性肿瘤中尤为重要。开发特异性的DNMT3A亚型抑制剂，以验证DNMT3A在某些疾病中的治疗潜力，是一个重要任务。在本综述中，我们总结了近年来发现的DNMT3A小分子抑制剂及其抑制活性，并根据抑制机制对其进行了分类。版权所有© Bentham Science Publishers；如有任何疑问，请发送电子邮件至epub@benthamscience.net。

DNA methyltransferase (DNMT) is a conserved family of Cytosine methylases, which plays a crucial role in the regulation of Epigenetics. They have been considered promising therapeutic targets for cancer. Among the DNMT family, mutations in the DNMT3A subtype are particularly important in hematologic malignancies. The development of specific DNMT3A subtype inhibitors to validate the therapeutic potential of DNMT3A in certain diseases is a significant task. In this review, we summarized the small molecule inhibitors of DNMT3A discovered in recent years and their inhibitory activities, and classified them based on their inhibitory mechanisms.Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.