Synthesis and characterization of quinazolinone derivatives against mammary carcinoma

Abstract

Aim

The present study was aimed to synthesis series of quinazolinone derivatives against mammary carcinoma.

Methods

The compounds were synthesized by reaction of nucleophilic attack, Wohler's classical synthesis followed by condensation reaction. The synthesized quinazolinone derivatives were characterized by physico chemical analysis like melting point, TLC, IR, UV and NMR. Compounds have been evaluated for their in-vitro antioxidant methods like DPPH method, H₂O₂ method, nitrous oxide scavenging method, super oxide scavenging method, ABTS radical scavenging, lipid peroxidation and also in-vitro cytotoxicity study against MCF-7, BT-549, ZR-75 (human breast cancer) cell lines by MTT assay method.

Results

From physico chemical data the structure of synthesized compounds was confirmed. Antioxidant activity was found from the IC₅₀ value. Qc showed lowest IC₅₀ value in DPPH radical scavenging assay and nitric oxide scavenging assay and was observed to be 27.20 μg/ml and 26.3 μg/ml respectively. In super oxide scavenging activity and lipid peroxidation and H₂O₂ assays showed a good activity it was observed 26.3 μg/ml, 18.10 μg/ml and 21.4 μg/ml respectively. Qb showed lowest IC₅₀ value in ABTS radical scavenging assay and was observed to be 26.9 μg/ml. Qe showed lowest IC₅₀ value in lipid peroxidation method and was observed to be 149 μg/ml. QN-D showed a moderate antioxidant. In cytotoxic activity, Qc showed lowest IC₅₀ value, i.e. 21.77, 23.03 and 21.14 μg/ml and Qb showed moderate values like 23.25 μg/ml, 27.39 μg/ml and 27.86 μg/ml in MCF-7, BT-549 and ZT-75 respectively.

Conclusion

All the synthesized compounds showed moderate to good antioxidant and potent cytotoxic activity.