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 memebered heterocyclic rings containing two 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. Presence of this nucleus in the 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 literature was 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 an important heterocyclic scaffolds with broad spectrum biological activities. They may be either mono substituted or disubstituted and 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 proved to be a helpful and vital tool for medicinal chemists investigating and working with 1,3,4-oxadiazoles and anticancer research programs.
Tyrosinase Inhibition, Antiglycation, and Antioxidant Activity of Xylocarpus granatum
