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This work is licensed under a Creative Commons Attribution 4.0 International License.
Synthesis and in vitro Cytotoxicity Study of Novel 4-Substituted Quinazolines Encompassed with Thiazolidinone and Azetidinone
Corresponding Author(s) : Gurubasavraj V. Pujar
Asian Journal of Chemistry,
Vol. 32 No. 10 (2020): Vol 32 Issue 10
Abstract
A series of quinazolines encompassed with thiazolidinone and azetidinone have been synthesized and evaluated for their antioxidant, anticancer and DNA binding studies. All the synthesized compounds were characterized by IR, 1H & 13C NMR and mass spectra. Antioxidant activity was carried out using % free radical scavenging by DPPH assay. Compounds 4b, 5b and 5d have shown better antioxidant activity (60, 67 and 66%, respectively) among the tested compounds. Compounds having % free radical scavenging activity more than 55% were evaluated for anticancer activity by MTT assay towards cell lines A-549 (lung carcinoma) and MDA-231 (human breast cancer). Results revealed that the tested compounds exhibited moderate to low anticancer activity. Further, DNA binding activity was studied by absorption titration method for all the synthesized compounds, and compound 5b showed a good binding constant of 70.05 and % hyperchromicity of 82.93%.
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A.A. Abdel-Aziz, L.A. Abou-Zeid, K.E. ElTahir, M.A. Mohamed, M.A. Abu El-Enin and A.S. El-Azab, Bioorg. Med. Chem., 24, 3818 (2016); https://doi.org/10.1016/j.bmc.2016.06.026
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S.J. von Niementowski, J. Prakt. Chem., 51, 564 (1894); https://doi.org/10.1002/prac.18950510150
S.M. Roopan, T. Maiyalagan and F.N. Khan, Can. J. Chem., 86, 1019 (2008); https://doi.org/10.1139/v08-149
T. Mosmann, J. Immunol. Methods, 65, 55 (1983); https://doi.org/10.1016/0022-1759(83)90303-4
L.L. Gundersen, J. Nissen-Meyer and B. Spilsberg, J. Med. Chem., 45, 1383 (2002); https://doi.org/10.1021/jm0110284
K.H. Chandramouli, K.N. Thimmaiah, A. Chandrashekar and C.J.M. D’Souza, Nucleos. Nucleot. Nucleic Acids, 23, 1639 (2004); https://doi.org/10.1081/NCN-200031461