title: Synthesis and in vitro antiproliferative evaluation of novel hybrids from 1,3,4-thiadiazole and benzisoselenazolone.
abstract: Novel hybrids from 1,3,4-thiadiazole and benzisoselenazolone were designed, synthesized and evaluated for their in vitro antiproliferative activities by CCK-8 assay against three types of human cancer cell lines, SMMC-7721, MCF-7 and A549 cells. The preliminary bioassay results demonstrated that all tested compounds 4a-p showed potent antiproliferative activities, and some compounds exhibited better effects than positive control ethaselen and 5-fluorouracil (5-FU) against various cancer cell lines. Furthermore, compound 4g showed significant antiproliferative activities against SMMC-7721 cells with an IC50 value of 2.08 µM. Compounds 4b and 4m displayed highly effective biological activities against MCF-7 cells with an IC50 values of 2.03 and 2.06 µM, respectively. Compound 4i exhibited the best inhibitory effect against A549 cells with an IC50 value of 1.03 µM.
authors.affiliation: School of Chemistry and Chemical Engineering, Tianjin University of Technology.
authors.forename: Fen
authors.initials: F
authors.lastname: Jing
authors.forename: Xiaoyun
authors.initials: X
authors.lastname: Fu
authors.forename: Sha
authors.initials: S
authors.lastname: Li
authors.forename: Baolin
authors.initials: B
authors.lastname: Li
authors.forename: Jijun
authors.initials: J
authors.lastname: Zhao
authors.forename: Xuefeng
authors.initials: X
authors.lastname: Wang
authors.forename: Yuming
authors.initials: Y
authors.lastname: Liu
authors.forename: Baoquan
authors.initials: B
authors.lastname: Chen
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001393:Azoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D004354:Drug Screening Assays, Antitumor; D005472:Fluorouracil / Q000494:pharmacology; D006801:Humans; D054833:Isoindoles; D061986:MCF-7 Cells; D009369:Neoplasms / Q000188:drug therapy*; D016566:Organoselenium Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013830:Thiadiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: C478160:(1,2-bis(1,2-benzisoselenazolone-3(2H)-ketone))ethane; D000970:Antineoplastic Agents; D001393:Azoles; D019086:Bridged Bicyclo Compounds, Heterocyclic; D054833:Isoindoles; D016566:Organoselenium Compounds; D013830:Thiadiazoles; C058949:1,3,4-thiadiazole; C042986:ebselen; D005472:Fluorouracil