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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

2

Graduate University of the Chinese Academy of Sciences, Beijing 100049, China

3

Gansu Key Laboratory of Preclinical Study for New Drugs, Institute of Pharmacology, School of Basic Medical Science, Lanzhou University, Lanzhou 730000, China

4

Institute of Biology, Gansu Academy of Sciences, Lanzhou 730000, China





*

Author to whom correspondence should be addressed.



Abstract 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





Autor: Mei Zhong 1,2, Yanjuan Liu 1,2, Junxi Liu 1,* , Duolong Di 1, Mengrou Xu 3, Yaya Yang 3, Wenguang Li 3, Yali Chen 3 and Jinxia Liu 4

Fuente: http://mdpi.com/



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