title: Synthesis and antitumor activities of novel hybrid molecules containing 1,3,4-oxadiazole and 1,3,4-thiadiazole bearing Schiff base moiety.
abstract: A series of novel hybrid molecules containing 1,3,4-oxadiazole and 1,3,4-thiadiazole bearing Schiff base moiety were designed, synthesized and evaluated for their in vitro antitumor activities against SMMC-7721, MCF-7 and A549 human tumor cell lines by CCK-8 assay. The bioassay results demonstrated that most of the tested compounds showed potent antitumor activities, and some compounds exhibited stronger effects than positive control 5-fluorouracil (5-FU) against various cell lines. Among these compounds, compound 8d showed the best inhibitory effect against SMMC-7721 cells, with IC50 value of 2.84 μM. Compounds 8k and 8 n displayed highly effective antitumor activities against MCF-7 cells, with IC50 values of 4.56 and 4.25 μM, respectively. Compounds 8a and 8 n exhibited significant antiproliferative activity against A549 cells, with IC50 values of 4.11 and 4.13 μM, respectively. The pharmacological results suggest that the substituents of phenyl ring on the 1,3,4-oxadiazole are vital for modulating antiproliferative activities against various tumor cell lines.
authors.affiliation: Department of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, PR China.
authors.forename: Kai
authors.initials: K
authors.lastname: Zhang
authors.affiliation: Department of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, PR China.
authors.forename: Peng
authors.initials: P
authors.lastname: Wang
authors.affiliation: Department of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, PR China.
authors.forename: Li-Na
authors.initials: LN
authors.lastname: Xuan
authors.affiliation: Department of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, PR China.
authors.forename: Xiao-Yun
authors.initials: XY
authors.lastname: Fu
authors.affiliation: Department of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, PR China.
authors.forename: Fen
authors.initials: F
authors.lastname: Jing
authors.affiliation: Department of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, PR China.
authors.forename: Sha
authors.initials: S
authors.lastname: Li
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. Electronic address: chenbaoquan66@126.com.
authors.forename: Bao-Quan
authors.initials: BQ
authors.lastname: Chen
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D049109:Cell Proliferation / Q000187:drug effects / Q000502:physiology; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D006801:Humans; D061986:MCF-7 Cells; D010069:Oxadiazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D012545:Schiff Bases / Q000138:chemical synthesis / Q000494:pharmacology; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D010069:Oxadiazoles; D012545:Schiff Bases; D013830:Thiadiazoles; C058949:1,3,4-thiadiazole; C583463:1,3,4-oxadiazole
keywords: 1,3,4-Oxadiazole; 1,3,4-Thiadiazole; Antitumor agents; Schiff base