Synthesis and anti-tumor activity of glycosyl oxadiazoles derivatives

  • Bioorg Med Chem Lett. 2014 Nov 15;24(22):5318-20. doi: 10.1016/j.bmcl.2014.09.042.
Kui Du  1 ,  Xianting Cao  1 ,  Pengfei Zhang  1 ,  Hui Zheng  1
Affiliations
  • 1. College of Material, Chemistry and Chemical Engineering, Hangzhou Normal University, Hangzhou 310016, China.
PMID: 25278236 DOI: 10.1016/j.bmcl.2014.09.042
Abstract

A new series of glycosyl oxadiazoles compounds were synthesized and characterized through (1)H NMR, (13)C NMR, IR and HRMS. The anti-tumor activities for MDA-MB-231 of all these new compounds were screened in vitro by MTT assay. Due to the modification of gastrodin analogues, the anti-tumor activities of these 1,3,4-oxadiazoles derivatives were greatly improved. Six compounds (6 c, 6 d, 6 i, 6 j, 6 k and 6 l) displayed relatively higher MDA-MB-231 potency with IC50 values (0.89, 0.26, 1.35, 3.60, 0.95 and 1.08 μM) compared with the reference medicine Rosiglitazone (5.23 μM).

Keywords
Anti-tumor activities; Gastrodin analogues; Heterocycles; Oxadiazoles derivatives.