2. Academic Validation
  3. Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives

Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives

  • Eur J Med Chem. 2019 Jul 1;173:213-227. doi: 10.1016/j.ejmech.2019.04.009.
Zefeng Zhao 1,  Huanhuan Song 2,  Jing Xie 1,  Tian Liu 1,  Xue Zhao 1,  Xufei Chen 1,  Xirui He 3,  Shaoping Wu 4,  Yongmin Zhang 5,  Xiaohui Zheng 6
Affiliations

Affiliations

  • 1 Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, Northwest University, 229 Taibai Road, Xi'an, 710069, China.
  • 2 Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, Northwest University, 229 Taibai Road, Xi'an, 710069, China; Biomedicine Key Laboratory of Shaanxi Province, Northwest University, Xi'an, Shaanxi, 710069, China.
  • 3 Honghui Hospital, Xi'an Jiaotong University, Xi'an, 710054, China.
  • 4 Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, Northwest University, 229 Taibai Road, Xi'an, 710069, China; Biomedicine Key Laboratory of Shaanxi Province, Northwest University, Xi'an, Shaanxi, 710069, China. Electronic address: [email protected].
  • 5 Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, Northwest University, 229 Taibai Road, Xi'an, 710069, China; Biomedicine Key Laboratory of Shaanxi Province, Northwest University, Xi'an, Shaanxi, 710069, China; Sorbonne Université, Institut Parisien de Chimie Moléculaire, CNRS UMR 8232, 4 place Jussieu, 75005, Paris, France.
  • 6 Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, Northwest University, 229 Taibai Road, Xi'an, 710069, China. Electronic address: [email protected].
PMID: 31009908 DOI: 10.1016/j.ejmech.2019.04.009
Abstract

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.

Keywords

3,4,5-Trimethoxycinnamic acid; Antimicrobial agents; Antitumor agents; Antiviral agents; CNS agnets; Hematologic agents; SAR; TMCA derivatives; anti-inflammatory agents.

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