Novel Triazolyl Berberine Derivatives Prepared via CuAAC Click Chemistry: Synthesis, Anticancer Activity and Structure-Activity Relationships

Author(s): Xin Jin , Lan Yan , Hong-jiao Li , Rui-Lian Wang , Zhen-Lin Hu , Yuan-Ying Jiang , Yong-Bing Cao , Tian-Hua Yan , Qing-Yan Sun .

Journal Name: Anti-Cancer Agents in Medicinal Chemistry

Volume 15 , Issue 1 , 2015

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Graphical Abstract:


To search for novel anticancer agents, we designed and synthesized a series of new triazolyl berberine derivatives. The evaluation of all the synthesized compounds and their anticancer activities against a panel of four human cancer cell lines including MCF-7 (breast), MCF-7/ADR (breast), SW-1990 (pancreatic), SMMC-7721 (liver) and the noncancer cell line HUVEC (human umbilical vein endothelial cell). The results showed that most of the compounds displayed better anticancer activities against MCF-7 and SMMC-7721 compared with berberine. Among these derivatives, compounds 5p and 5a exhibited the most potent inhibitory activities against the SMMC-7721 and SW-1990 cell lines with IC50 values of 14.861 ± 2.4 µM and 16.798 ± 3.4 µM. Furthermore, compounds 5p, 5a and 5n exhibited much better selectivity toward the normal cell line HUVEC than berberine.

Keywords: Anticancer, berberine, click chemistry, structure-activity relationship.

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Article Details

Year: 2015
Page: [89 - 98]
Pages: 10
DOI: 10.2174/1871520614666141203142012

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