Synthesis and Evaluation of Anticancer Activity of 1, 3, 4-Oxadiazole Derivatives against Ehrlich Ascites Carcinoma Bearing Mice and Their Correlation with Histopathology of Liver

Abstract

A series of 2, 5-disubstituted 1, 3, 4-Oxadiazole derivatives (4A-4G) have been synthesized with the help of different aromatic benzaldehyde and final compounds were characterized by FT-IR, 1 H NMR and Mass spectroscopy. The anticancer study was investigated against Ehrlich Ascites Carcinoma (EAC) bearing albino mice. The synthesized (4A-4G) compounds were administered intraperitoneally at dose of 20-25 mg/kg; body weight per day for 7 days after 24 hour of tumor inoculation in mice. The standard compound used was 5-FU (20 mg/kg; body, weight). Synthesized compounds (4A-4G) remarkably decreased the body weight, tumor volume, packed cell volume, viable cell count and increased in tumor weight (%) inhibition, tumor cells (%) inhibition, the life span, nonviable cell count of EAC tumor bearing mice when compared with the control group. The liver section of EAC treated control group (II) was compared with the drug treated groups (III-X). The histopathological observations of test groups suggested that normal architecture of liver nucleus, parenchyma, and hepatic cells were regenerated, which was damaged in EAC control group. All the synthesized compounds (4A-4G) showed significant anticancer activity in EAC bearing mice which encourages us to develop/improve similar other compounds and test them for their anticancer activity.

Novel 1,3,4-oxadiazole Targets STAT3 Signaling to Induce Antitumor Effect in Lung Cancer

“…Moreover, CHK9 did not exhibit toxicity up to 20 mg/kg body weight in the tested animals. 1,3,4-oxadiazoles have displayed similar toxicity profiles in the previous in vitro and in vivo studies [ 55 , 56 ]. A limited number of studies have demonstrated the in vivo antitumor activity of oxadiazoles.…”

1,3,4‐oxadiazole and its derivatives: A review on recent progress in anticancer activities

“…A Monte Carlo Simulations studies suggested that the schiff bases containing the >C=N group possessed antitumor activity (Guimaráes et al, 2005). In this context, Roy et al (2017) designed and reported 1,3,4-oxadiazole containing >C=N group at its 2 position. The researchers synthesized new 2,5-disubstituted-1,3,4-oxadiazole derivatives and studied their anticancer activity and histopathological study of the liver was performed.…”

Synthesis and Biological Activities of 1, 3, 4-Oxadiazole Derivatives: A Review of Literature.

“…The fluorescence properties of all the compounds were analysed in dimethyl sulfoxide media and were evaluated for their n vitro inhibitory activity against commercial enzyme xanthine oxidase (XO) by measuring the formation of uric acid from xanthine. [17] (2017) were synthesised some novel 2, 5-Disubstituted 1, 3, 4-Oxadiazole derivatives (scheme: 20) using different aromatic benzaldehyde, and evaluated for their anticancer activity against Ehrlich Ascites Carcinoma (EAC) bearing albino mice. …”