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Anti-Cancer Agents in Medicinal Chemistry


ISSN (Print): 1871-5206
ISSN (Online): 1875-5992

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 and Qing-Yan Sun

Volume 15, Issue 1, 2015

Page: [89 - 98] Pages: 10

DOI: 10.2174/1871520614666141203142012

Price: $65


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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