Background: Oxadiazole emerged as an important class of heterocyclic compound with
diverse biological activities like anticancer, antitubercular, anticonvulsant, anti-tubulin, antimicrobial,
anti-inflammatory, antioxidant etc.
Objective: The objective of this study is to synthesis series of twelve substituted N-[(1,3,4-oxadiazol-2-
yl)methyl]benzamines (6a-l) and their evaluation as antiproliferative and antioxidant agents.
Methods: The substituted N-[(1,3,4-oxadiazol-2-yl)methyl]benzamines (6a-l) analogues were synthesized
as per the reported procedure. The antiproliferative activity was tested against nine different
panels cancer cell lines (leukemia, colon, renal, non-small cell lung, breast, CNS, melanoma, prostate,
and ovarian cancer) at 10 µM drug concentrations as per the NCI US Protocol.
Results: 2-(5-((3-Chloro-4-fluorophenylamino)methyl)-1,3,4-oxadiazol-2-yl)phenol (6e) revealed
the significant antiproliferative activity among the series of title compounds (6a-l). The compound,
6e showed maximum sensitivity towards CCRF-CEM, MCF-7, MOLT-4, T-47D, and SR cell lines
with percent growth inhibitions (%GIs) of 79.92, 56.67, 39.62, 34.71 and 33.35, respectively. Furthermore,
the compounds, 6e and 6c showed promising antioxidant activity with an IC50 value of
15.09 and 19.02 µM, respectively in DPPH free radicals (FR) scavenging activity.
Conclusion: The present study may support a significant value in cancer drug discovery programme.