Department of Pharmaceutical Technology and Chemistry, University of Navarra, E-31008 Pamplona, Spain.
Department of Pharmacology, Penn State Cancer Institute, CH72, Penn State College of Medicine, 500 University Drive, Hershey, Pennsylvania 17033, United States.
J Med Chem. 2023 Mar 23;66(6):3703-3731. doi: 10.1021/acs.jmedchem.2c01406. Epub 2023 Mar 1.
Since the beginning of history, natural products have been an abundant source of bioactive molecules for the treatment of different diseases, including cancer. Many allyl derivatives, which have shown anticancer activity both and in a large number of cancers, are bioactive molecules found in garlic, cinnamon, nutmeg, or mustard. In addition, synthetic products containing allyl fragments have been developed showing potent anticancer properties. Of particular note is the allyl derivative 17-AAG, which has been evaluated in Phase I and Phase II/III clinical trials for the treatment of multiple myeloma, metastatic melanoma, renal cancer, and breast cancer. In this Perspective, we compile extensive literature evidence with descriptions and discussions of the most recent advances in different natural and synthetic allyl derivatives that could generate cancer drug candidates in the near future.
自历史之初,天然产物一直是治疗包括癌症在内的各种疾病的生物活性分子的丰富来源。许多烯丙基衍生物在大量癌症中表现出抗癌活性,是大蒜、肉桂、肉豆蔻或芥末中发现的生物活性分子。此外,还开发了含有烯丙基片段的合成产品,显示出强大的抗癌特性。特别值得注意的是烯丙基衍生物 17-AAG,它已在 I 期和 II/III 期临床试验中进行了评估,用于治疗多发性骨髓瘤、转移性黑色素瘤、肾癌和乳腺癌。在本观点中,我们汇编了广泛的文献证据,描述和讨论了不同天然和合成烯丙基衍生物的最新进展,这些进展可能在不久的将来产生癌症药物候选物。