1. Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives
- Author
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Xirui He, Huanhuan Song, Zefeng Zhao, Yongmin Zhang, Shaoping Wu, Xufei Chen, Tian Liu, Jing Xie, Xue Zhao, Xiaohui Zheng, Key Laboratory of Resource Biology and Biotechnology, Northwest University, Xi'an, Glycochimie Organique Biologique et Supramoléculaire (GOBS), Institut Parisien de Chimie Moléculaire (IPCM), Chimie Moléculaire de Paris Centre (FR 2769), Institut de Chimie du CNRS (INC)-École normale supérieure - Paris (ENS Paris), Université Paris sciences et lettres (PSL)-Université Paris sciences et lettres (PSL)-Centre National de la Recherche Scientifique (CNRS)-Ecole Nationale Supérieure de Chimie de Paris - Chimie ParisTech-PSL (ENSCP), Université Paris sciences et lettres (PSL)-Ecole Superieure de Physique et de Chimie Industrielles de la Ville de Paris (ESPCI Paris), Université Paris sciences et lettres (PSL)-Université Pierre et Marie Curie - Paris 6 (UPMC)-Institut de Chimie du CNRS (INC)-École normale supérieure - Paris (ENS Paris), Université Paris sciences et lettres (PSL)-Université Pierre et Marie Curie - Paris 6 (UPMC)-Sorbonne Université (SU)-Centre National de la Recherche Scientifique (CNRS)-Chimie Moléculaire de Paris Centre (FR 2769), and Université Paris sciences et lettres (PSL)-Université Pierre et Marie Curie - Paris 6 (UPMC)-Sorbonne Université (SU)-Centre National de la Recherche Scientifique (CNRS)
- Subjects
CNS agnets ,POLE 3 ,Hematologic agents ,Druggability ,Antineoplastic Agents ,Antiviral Agents ,01 natural sciences ,Article ,anti-inflammatory agents ,03 medical and health sciences ,Drug Discovery ,TMCA derivatives ,[CHIM]Chemical Sciences ,030304 developmental biology ,Pharmacology ,3,4,5-Trimethoxycinnamic acid ,0303 health sciences ,Antitumor agents ,Molecular Structure ,010405 organic chemistry ,Drug discovery ,Chemistry ,Anti-Inflammatory Agents, Non-Steroidal ,Organic Chemistry ,Biological activity ,General Medicine ,Antimicrobial agents ,Combinatorial chemistry ,Anti-Bacterial Agents ,3. Good health ,0104 chemical sciences ,GOBS ,Cinnamates ,Central Nervous System Agents ,SAR - 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., Graphical abstract Image 1, Highlights • 3,4,5-Trimethoxycinnamic acid (TMCA) derivatives show applications in different pathophysiological conditions due to its privileged structural scaffolds. • Natural derived TMCA analogues and chemically modified TMCA ester and amide analogues and their bioactivities are focused in this review. Additionally, it also comprehensively summarized the relationship of significant biological activities along with SAR studies of synthetic TMCA derivatives.
- Published
- 2019