title: Novel Triazolyl berberine derivatives prepared via CuAAC click chemistry: Synthesis, Anticancer Activity and Structure-Activity Relationships.
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 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.
authors.forename: Xin
authors.initials: X
authors.lastname: Jin
authors.forename: Lan
authors.initials: L
authors.lastname: Yan
authors.forename: Hong-Jiao
authors.initials: HJ
authors.lastname: Li
authors.forename: Rui-Lian
authors.initials: RL
authors.lastname: Wang
authors.forename: Zhen-Lin
authors.initials: ZL
authors.lastname: Hu
authors.forename: Yuan-Ying
authors.initials: YY
authors.lastname: Jiang
authors.forename: Yong-Bing
authors.initials: YB
authors.lastname: Cao
authors.forename: Tian-Hua
authors.initials: TH
authors.lastname: Yan
authors.affiliation: School of Pharmacy, Second Military Medical University, Shanghai 200433, China. sqy_2000@163.com.
authors.forename: Qing-Yan
authors.initials: QY
authors.lastname: Sun