Oxadiazoles as privileged motifs for promising anticancer leads: recent advances and future prospects

Arch Pharm (Weinheim). 2014 Jan;347(1):1-20. doi: 10.1002/ardp.201300231. Epub 2013 Nov 22.

Abstract

Taking into account the rising trend of the incidence of cancers of various organs, effective therapies are urgently needed to control human malignancies. The rapid emergence of hundreds of new agents that modulate an ever-growing list of cancer-specific molecular targets offers tremendous hope for cancer patients. However, almost all of the chemotherapy drugs currently on the market cause serious side effects. Based on these facts, the design of new chemical entities as anticancer agents requires the simulation of a suitable bioactive pharmacophore. The pharmacophore not only should have the required potency but must also be safer on normal cell lines than on tumor cells. In this perspective, oxadiazole scaffolds with well-defined anticancer activity profile have fueled intense academic and industrial research in recent years. This paper is intended to highlight the recent advances along with current developments as well as future outlooks for the design of novel and efficacious anticancer agents based on oxadiazole motifs.

Keywords: Cancer chemotherapy; Cytotoxicity; Heterocycles; Inhibition; Oxadiazoles.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / toxicity
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Dose-Response Relationship, Drug
  • Drug Design*
  • Drug Discovery / trends*
  • Forecasting*
  • Humans
  • Inhibitory Concentration 50
  • Molecular Structure
  • Oxadiazoles / chemistry*
  • Oxadiazoles / pharmacology*
  • Oxadiazoles / toxicity
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Oxadiazoles