title: Synthesis and antiproliferative evaluation of novel 1,2,4-triazole derivatives incorporating benzisoselenazolone scaffold.
abstract: A series of novel 1,2,4-triazole derivatives incorporating benzisoselenazolone scaffold were designed, synthesized and evaluated for their in vitro antiproliferative activities against human cancer cell lines SMMC-7721, Hela, A549, and normal cell lines L929 by CCK-8 assay. The preliminary bioassay results demonstrated that most of the tested compounds 3a-3n exhibited antiproliferation with different degrees, and some compounds showed better effects than positive controls ethaselen and 5-fluorouracil (5-FU) against various cancer cell lines. Among these compounds, compounds 3b and 3c displayed highly effective biological activities against SMMC-7721cells with IC50 values of 6.02 and 6.01 μM, respectively. Compound 3n showed significant antiproliferative activities against Hela cells with IC50 value of 3.94 μM. Compound 3n exhibited the best inhibitory effect against A549 cells with IC50 value 9.14 μM. Furthermore, most of the tested compounds showed weak cytotoxic effect against the normal cell lines L929. The pharmacological results suggest that the substituent groups are vital for improving the potency and selectivity of this class of compounds.
authors.affiliation: Department of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, PR China.
authors.forename: Bao-Lin
authors.initials: BL
authors.lastname: Li
authors.affiliation: Department of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, PR China.
authors.forename: Bo
authors.initials: B
authors.lastname: Li
authors.affiliation: Department of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, PR China.
authors.forename: Rui-Lian
authors.initials: RL
authors.lastname: Zhang
authors.affiliation: Department of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, PR China.
authors.forename: Ji-Jun
authors.initials: JJ
authors.lastname: Zhao
authors.affiliation: Department of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, PR China.
authors.forename: Xue-Feng
authors.initials: XF
authors.lastname: Wang
authors.affiliation: Department of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, PR China.
authors.forename: Yu-Ming
authors.initials: YM
authors.lastname: Liu
authors.affiliation: Department of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, PR China.
authors.forename: Yan-Ping
authors.initials: YP
authors.lastname: Shi
authors.affiliation: Department of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, PR China.
authors.forename: Jin-Biao
authors.initials: JB
authors.lastname: Liu
authors.affiliation: Department of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, PR China. Electronic address: chenbaoquan66@126.com.
authors.forename: Bao-Quan
authors.initials: BQ
authors.lastname: Chen
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000737:chemistry; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D005472:Fluorouracil / Q000494:pharmacology; D006367:HeLa Cells; D006801:Humans; D016566:Organoselenium Compounds / Q000737:chemistry; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
chemical_list: C478160:(1,2-bis(1,2-benzisoselenazolone-3(2H)-ketone))ethane; D000970:Antineoplastic Agents; D019086:Bridged Bicyclo Compounds, Heterocyclic; D016566:Organoselenium Compounds; D014230:Triazoles; C045575:1,2,4-triazole; D005472:Fluorouracil
keywords: 1,2,4-Triazole derivatives; Antiproliferative activity; Benzisoselenazolone; Ebselen; Ethaselen