Huang Ying, Li Gen, Hong Chong, Zheng Xia, Yu Haiyang, Zhang Yan
Key Laboratory of Computational Chemistry-Based Natural Antitumor Drug Research & Development, Liaoning Province, School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang, China.
School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Tianjin, China.
Front Oncol. 2021 Sep 20;11:733369. doi: 10.3389/fonc.2021.733369. eCollection 2021.
Steroidal alkaloids contain both steroidal and alkaloid properties in terms of chemical properties and pharmacological activities. Due to outstanding biological activities such as alkaloids and similar pharmacological effects to other steroids, steroidal alkaloids have received special attention in anticancer activity recently. Substituted groups in chemical structure play markedly important roles in biological activities. Therefore, the effective way to obtain lead compounds quickly is structural modification, which is guided by structure-activity relationships (SARs). This review presents the SAR of steroidal alkaloids and anticancer, including pregnane alkaloids, cyclopregnane alkaloids, cholestane alkaloids, C-nor-D-homosteroidal alkaloids, and bis-steroidal pyrazine. A summary of SAR can powerfully help to design and synthesize more lead compounds.
甾体生物碱在化学性质和药理活性方面兼具甾体和生物碱的特性。由于甾体生物碱具有诸如生物碱类的显著生物活性以及与其他甾体相似的药理作用，其在抗癌活性方面最近受到了特别关注。化学结构中的取代基在生物活性中起着极为重要的作用。因此，以构效关系（SARs）为指导进行结构修饰是快速获得先导化合物的有效途径。本综述介绍了甾体生物碱的构效关系及其抗癌作用，包括孕烷生物碱、环孕烷生物碱、胆甾烷生物碱、C-去甲-D-高甾体生物碱和双甾体吡嗪。构效关系的总结能够有力地帮助设计和合成更多的先导化合物。
