Recent progress on triterpenoid derivatives and their anticancer potential

• Published in: Phytochemistry (Oxford) Vol. 229; p. 114257
• Main Authors: Zhao, Zi-Xuan, Zou, Qiong-Yu, Ma, Ying-Hong, Morris‐Natschke, Susan L., Li, Xiang-Yuan, Shi, Lin-Chun, Ma, Guo-Xu, Xu, Xu‐Dong, Yang, Mei‐Hua, Zhao, Zi-Jian, Li, Yuan-Xiang, Xue, Jing, Chen, Chin-Ho, Wu, Hai-Feng
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 01.01.2025
• Subjects: Anticancer activity; Molecular simulation; Natural products; Structure-activity relationship; Synthesis; Triterpenoid; Molecular simulation; Synthesis; Triterpenoid; Natural products; Structure-activity relationship; Anticancer activity
• ISSN: 0031-9422; 1873-3700; 1873-3700
• DOI: 10.1016/j.phytochem.2024.114257

Cancer poses a significant global public health challenge, with commonly used adjuvant or neoadjuvant chemotherapy often leading to adverse side effects and drug resistance. Therefore, advancing cancer treatment necessitates the ongoing development of novel anticancer agents with diverse structures and mechanisms of action. Natural products remain crucial in the process of drug discovery, serving as a primary source for pharmaceutical leads and therapeutic advancements. Triterpenoids are particularly compelling due to their complex structures and wide array of biological activities. Recent research has demonstrated that naturally occurring triterpenes and their derivatives have the potential to serve as promising candidates for new drug development. This review aims to comprehensively explore the anticancer properties of triterpenoids and their synthetic analogs, with a focus on recent advancements. Various aspects, such as synthesis, phytochemistry, and molecular simulation for structure-activity relationship analyses, are summarized. It is anticipated that triterpenoid derivatives will emerge as notable anticancer agents following further investigation into their mechanisms of action and in vivo studies. [Display omitted] •More than 1000 triterpenoids with cytotoxicity were reviewed from 2016 to 2023.•Anticancer betulinic and oleanolic acid derivatives were thoroughly examined.•Cytotoxic triterpenoids with recently published skeletons were described.•Utilization of network pharmacology and molecular simulations were discussed.