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 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.
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
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D001599:Berberine / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D045744:Cell Line, Tumor; D057930:Click Chemistry / Q000379:methods; D015195:Drug Design; D061307:Human Umbilical Vein Endothelial Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D061986:MCF-7 Cells; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D001599:Berberine