Limonene and perillyl alcohol are natural monoterpenes that have attracted the attention of medicinal chemists due to their promising anticancer activities. Considering this, both compounds were explored as scaffolds to obtain various derivatives with anticancer activity. In this review, the data are organized for the first time, with a focus on the synthetic methods and strategies to obtain the derivatives throughout the period from 2000 to 2020. A brief discussion regarding the structure and activity relationships of the most active derivatives, stereoisomers, and their mechanisms of action is presented. Among the active compounds, a series of limonenes with thiosemicarbazone groups and perillyl alcohol hybrids with glycosides or drugs are illustrated. Taking all of this into account, this review may help researchers develop new promising anticancer candidates based on the structures of limonene and perillyl alcohol.

柠檬烯和紫苏醇是天然单萜类化合物，因其具有良好的抗癌活性而受到药物化学家的关注。考虑到这一点，这两种化合物都作为支架进行了探索，以获得具有抗癌活性的各种衍生物。本次综述首次整理了数据，重点介绍了2000年至2020年期间获得衍生物的合成方法和策略。 简要讨论了最活跃的衍生物、立体异构体的结构和活性关系，并介绍了它们的作用机制。在活性化合物中，举例说明了一系列带有缩氨基硫脲基团的柠檬烯和紫苏醇与糖苷或药物的杂化物。考虑到这一切，