Design and synthesis of cinnamic acid triptolide ester derivatives as potent antitumor agents and their biological evaluation

Bioorg Med Chem Lett. 2022 Jul 1:67:128760. doi: 10.1016/j.bmcl.2022.128760.

Chenglong Cheng ¹, Gudong Li ¹, Guojun Zheng ², Changyuan Yu ³

Affiliations

1 College of Life Science and Technology, Beijing University of Chemical Technology, Beijing 100029, People's Republic of China.
2 College of Life Science and Technology, Beijing University of Chemical Technology, Beijing 100029, People's Republic of China. Electronic address: zhenggj@mail.buct.edu.cn.
3 College of Life Science and Technology, Beijing University of Chemical Technology, Beijing 100029, People's Republic of China. Electronic address: yucy@mail.buct.edu.cn.

PMID: 35476958 DOI: 10.1016/j.bmcl.2022.128760

Abstract

A series of novel cinnamic acid triptolide ester derivatives were synthesized, and their growth inhibitory properties against human hepatoma HepG2 cells were assessed as the measure of cytotoxicity with triptolide as the positive control. One of the phenolic hydroxyl phosphorylated products, CL20 was found to possess the best cytotoxicity and surpassed the parent natural triptolide, suggesting that compound CL20 is a promising antitumor lead compound and deserves further research of pharmacological activity. In addition, the structure-activity relationship for these compounds was also investigated.

Keywords

Cinnamic acid; Cytotoxicity; Structure-activity relationships; Synthesis; Triptolide.

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