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

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


Volume 16, 12 Issues, 2016


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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Editor-in-Chief:
Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
France


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



Anti-Cancer Agents in Medicinal Chemistry, 15(1): 89-98.

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.

Affiliation: School of Pharmacy, Second Military Medical University, Shanghai 200433, China.

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

Volume: 15
Issue Number: 1
First Page: 89
Last Page: 98
Page Count: 10
DOI: 10.2174/1871520614666141203142012
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