Cyclic dinucleotides (CDNs) have been recognized as second messengers in both prokaryotes and eukaryotes. Until now, four CDNs were identified in the natural organism. In mammalian cells, CDNs could activate stimulator of interferon genes (STING), leading to the induction of type I interferon pro-inflammatory cytokines. It indicated that CDNs could be used for the treatment of tumor and infectious diseases in immune-therapy. Here, we will review the latest progress of the CDNs analogs and their bioactivities. What’s more, the preparation of CDNs through biosynthetic and chemical synthetic methods was summarized as well. It was hoped that this review would provide a comprehensive understanding of CDNs based STING agonists on the chemical perspective for readers who are interested in this area.

环二核苷酸（CDN）在原核生物和真核生物中均被认为是第二信使。到目前为止，在自然生物中已鉴定出四个CDN。在哺乳动物细胞中，CDN可以激活干扰素基因的刺激物（STING），从而导致I型干扰素促炎细胞因子的诱导。表明CDNs可用于免疫治疗中的肿瘤和感染性疾病。在这里，我们将回顾CDNs类似物及其生物活性的最新进展。此外，还总结了通过生物合成和化学合成方法制备CDN的方法。希望这篇综述能够为对这一领域感兴趣的读者提供基于CDNs的STING激动剂的化学观点的全面理解。