1,3,4-Oxadiazole Containing Compounds As Therapeutic Targets For Cancer Therapy

Abstract

Background: Cancer is the first or second leading cause of premature death in 134 of 183 countries in the world. 1,3,4-Oxadiazoles are five membered heterocyclic rings containing nitrogen (two atoms) and oxygen (one atom). They show better thermal stability, metabolic stability, aqueous solubility, and lower lipophilicity than the other isomeric oxadiazoles. They are important class of heterocycles present in many drug structures like Raltegravir, Furamizole Tidazosin, Nesapidil, Setileuton (MK-0633) and Zibotentan. The presence of this nucleus in therapeutics has made them an indispensable anchor for drug design and development. Several 1,3,4-oxadiazoles are prepared and reported as anticancer agents by numerous scientists worldwide.

Objectives: The present review discusses the anticancer potentials together with the molecular targets of 1,3,4-oxadiazoles reported since 2010. The Structure-Activity Relationship (SAR) and molecular docking simulation on different targets have also been discussed herein. Some of the important cancer targets have also been explored.

Methods: The most potent 1,3,4-oxadiazoles reported in the literature were highlighted in the manuscript. The anticancer activity was reported in terms of Growth Percent (GP), percent growth inhibition (%GI), GI₅₀, IC₅₀, and LC₅₀; and TGI.

Results: 1,3,4-Oxadiazoles are important heterocyclic scaffolds with broad spectrum biological activities. They may be either mono substituted or disubstituted, and they may act as an indispensable anchor for drug design and discovery due to their thermal stability together with low lipophilicity. They exhibited anticancer potentials and showed the inhibitions of various cancer targets.

Conclusion: The discussion outlined herein will prove to be a helpful and vital tool for medicinal chemists investigating and working with 1,3,4-oxadiazoles and anticancer research programs.

Keywords: 1,3,4-Oxadiazoles; Anticancer; Molecular docking.; antiproliferative; cytotoxicity; structure activity relationship (SAR).