2. Academic Validation
  3. Synthesis and antitumor activities of novel hybrid molecules containing 1,3,4-oxadiazole and 1,3,4-thiadiazole bearing Schiff base moiety

Synthesis and antitumor activities of novel hybrid molecules containing 1,3,4-oxadiazole and 1,3,4-thiadiazole bearing Schiff base moiety

  • Bioorg Med Chem Lett. 2014 Nov 15;24(22):5154-6. doi: 10.1016/j.bmcl.2014.09.086.
Kai Zhang 1,  Peng Wang 1,  Li-Na Xuan 1,  Xiao-Yun Fu 1,  Fen Jing 1,  Sha Li 1,  Yu-Ming Liu 1,  Bao-Quan Chen 2
Affiliations

Affiliations

  • 1 Department of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, PR China.
  • 2 Department of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, PR China. Electronic address: chenbaoquan66@126.com.
PMID: 25442303 DOI: 10.1016/j.bmcl.2014.09.086
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.

Keywords

1,3,4-Oxadiazole; 1,3,4-Thiadiazole; Antitumor agents; Schiff base.

Figures