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Molecules 2014, 19(8), 12099-12115;

Isocorydine Derivatives and Their Anticancer Activities

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
Graduate University of the Chinese Academy of Sciences, Beijing 100049, China
Gansu Key Laboratory of Preclinical Study for New Drugs, Institute of Pharmacology, School of Basic Medical Science, Lanzhou University, Lanzhou 730000, China
Institute of Biology, Gansu Academy of Sciences, Lanzhou 730000, China
Author to whom correspondence should be addressed.
Received: 5 June 2014 / Revised: 13 July 2014 / Accepted: 22 July 2014 / Published: 12 August 2014
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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. View Full-Text
Keywords: aporphine alkaloids; isocorydine; synthesis; anticancer activity aporphine alkaloids; isocorydine; synthesis; anticancer activity

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Zhong, M.; Liu, Y.; Liu, J.; Di, D.; Xu, M.; Yang, Y.; Li, W.; Chen, Y.; Liu, J. Isocorydine Derivatives and Their Anticancer Activities. Molecules 2014, 19, 12099-12115.

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