癌症构成了重大的全球公共卫生挑战，常用的辅助或新辅助化疗通常会导致不良副作用和耐药性。因此，推进癌症治疗需要不断开发具有不同结构和作用机制的新型抗癌药物。天然产物在药物发现过程中仍然至关重要，是药物先导化合物和治疗进展的主要来源。三萜类化合物因其复杂的结构和广泛的生物活性而特别引人注目。最近的研究表明，天然存在的三萜及其衍生物有潜力成为新药开发的有希望的候选者。本综述旨在全面探讨三萜类化合物及其合成类似物的抗癌特性，重点关注最新进展。总结了合成、植物化学和构效关系分析的分子模拟等各个方面。经过进一步研究其作用机制和体内研究，预计三萜衍生物将成为著名的抗癌药物。版权所有 © 2024。由 Elsevier Ltd 出版。

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.Copyright © 2024. Published by Elsevier Ltd.