TMCA (3,4,5-trimethoxycinnamic acid) ester and amide are privileged structural scaffolds in drug discovery which are widely distributed in natural products and consequently produced diverse therapeutically relevant pharmacological functions. Owing to the potential of TMCA ester and amide analogues as therapeutic agents, researches on chemical syntheses and modifications have been carried out to drug-like candidates with broad range of medicinal properties such as antitumor, antiviral, CNS (central nervous system) agents, antimicrobial, anti-inflammatory and hematologic agents for a long time. At the same time, SAR (structure-activity relationship) studies have draw greater attention among medicinal chemists, and many of the lead compounds were derived for various disease targets. However, there is an urgent need for the medicinal chemists to further exploit the precursor in developing chemical entities with promising bioactivity and druggability. This review concisely summarizes the synthesis and biological activity for TMCA ester and amide analogues. It also comprehensively reveals the relationship of significant biological activities along with SAR studies.

TMCA（3,4,5-三甲氧基肉桂酸）酯和酰胺是药物发现中的特殊结构支架，广泛分布于天然产物中，因此产生多种与治疗相关的药理功能。由于TMCA的潜力酯和酰胺类似物作为治疗剂，对具有广泛药用特性的类药候选物进行了化学合成和修饰研究，如抗肿瘤、抗病毒、CNS（中枢神经系统）药物、抗菌、抗炎和血液学长期代理。与此同时，SAR（结构-活性关系）研究引起了药物化学家的更多关注，许多先导化合物被衍生用于各种疾病靶点。然而，药物化学家迫切需要进一步利用前体来开发具有良好生物活性和成药性的化学实体。本综述简要总结了TMCA的合成和生物活性酯和酰胺类似物。它还全面揭示了重大生物活动与 SAR 研究的关系。