Abstract
The current study was chiefly designed to examine the antiproliferative and antioxidant activities of some novel quinazolinone(thione) derivatives 6–14. The present work focused on two main points; firstly, comparing between quinazolinone and quinazolinthione derivatives. Whereas, antiproliferative (against two cell lines namely, HepG2 and MCF-7) and antioxidant (by two methods; ABTS and DPPH) activities of the investigated compounds, the best quinazolinthione derivatives were 6 and 14, which exhibited excellent potencies comparable to quinazolinone derivatives 5 and 9, respectively. Secondly, we compared the activity of four series of Schiff bases which included the quinazolinone moiety (11a–d). In addition, the antiproliferative and antioxidant activities of the compounds with various aryl aldehyde hydrazone derivatives (11a–d) analogs were studied. The compounds exhibited potency that increased with increasing electron donating group in p-position (OH > OMe > Cl) due to extended conjugated systems. Noteworthy, most of antiproliferative and antioxidant activities results for the tested compounds are consistent with the DFT calculations.
Highlights
Cancer is the second leading cause of death globally, and the contribution of cancer disease to the overall mortality rate is increasing
One of the aims of this work is the screening of all synthesized compounds for antioxidant activity different methods, of all namely
13 C-NMR spectra were performed at chemical warfare labs, Egypt, with a Varian Gemini spectra were performed at chemical warfare labs, Egypt, with a Varian Gemini spectrometer (Metrohim, California, United States) in DMSO-d6 as a solvent by using tetramethylsilane (TMS) as a reference
Summary
Cancer is the second leading cause of death globally, and the contribution of cancer disease to the overall mortality rate is increasing.
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