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

Autor: Xin Jin, Tianhua Yan, Zhen-Lin Hu, Yong-Bing Cao, Li Hongjiao, Qingyan Sun, Rui-Lian Wang, Lan Yan, Yuanying Jiang
Rok vydání: 2014
Předmět:
Zdroj: Anti-Cancer Agents in Medicinal Chemistry. 15:89-98
ISSN: 1871-5206
DOI: 10.2174/1871520614666141203142012
Popis: 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 non-cancer 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.
Databáze: OpenAIRE