Isocorydine Derivatives and Their Anticancer Activities

Molecules

Mei Zhong¹  Yanjuan Liu¹  Junxi Liu¹  Duolong Di¹  Mengrou Xu²  Yaya Yang²  Wenguang Li²  Yali Chen² 

[1] Key Laboratory of Chemistry of Northwestern Plant Resources and Key Laboratory for Natural Medicine of Gansu Province, Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences, Lanzhou 730000, China; E-Mails:;Gansu Key Laboratory of Preclinical Study for New Drugs, Institute of Pharmacology, School of Basic Medical Science, Lanzhou University, Lanzhou 730000, China; E-Mails:

关键词: aporphine alkaloids;    isocorydine;    synthesis;    anticancer activity;   

DOI  :  10.3390/molecules190812099

来源: mdpi

【 摘 要 】

In order to improve the anticancer activity of isocorydine (ICD), ten isocorydine derivatives were prepared through chemical structure modifications, and their in vitro and in vivo activities were experimentally investigated. 8-Amino-isocorydine (8) and 6a,7-dihydrogen-isocorydione (10) could inhibit the growth of human lung (A549), gastric (SGC7901) and liver (HepG2) cancer cell lines in vitro. Isocorydione (2) could inhibit the tumor growth of murine sarcoma S₁₈₀-bearing mice, and 8-acetamino-isocorydine (11), a pro-drug of 8-amino-isocorydine (8), which is instable in water solution at room temperature, had a good inhibitory effect on murine hepatoma H₂₂-induced tumors. The results suggested that the isocorydine structural modifications at C-8 could significantly improve the biological activity of this alkaloid, indicating its suitability as a lead compound in the development of an effective anticancer agent.

【 授权许可】

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© 2014 by the authors; licensee MDPI, Basel, Switzerland.