Synthesis and biological evaluation of novel oxadiazole derivatives: A new class of thymidine phosphorylase inhibitors as potential anti-tumor agents

Abstract

Based on the fact that the thymidine phosphorylase inhibitors are considered potential anti-tumor agents, a range of novel oxadiazole derivatives 3a-3u was designed and synthesized by a simple and facile synthetic route The biological assay revealed that majority of compounds displayed modest inhibitory activity against thymidine phosphorylase at low micromolar concentrations (IC50 173.23 ± 3.04 to 14.40 ± 2.45 μM) In the current study the most active compounds were 3h and 3q with IC50 values 14.40 ± 2.45 and 17.60 ± 1.07 μM, respectively Molecular docking studies were performed on the most active compounds (3h, 3k, 3o-3q) to show their binding mode © 2014 Elsevier Ltd All rights reserved.