Inhibiting Cyclin-dependent kinase 2 (CDK2) has been established as a therapeutic strategy for the treatment of many cancers. Accordingly, this study aimed at developing a new set of quinazolinone-based derivatives as CDK2 inhibitors. The new compounds were evaluated for their anticancer activity against sixty tumour cell lines. Compounds
5c
and
8a
showed excellent growth inhibition against the melanoma cell line MDA-MB-435 with GI% of 94.53 and 94.15, respectively. Cell cycle analysis showed that compound
5c
led to cell cycle cessation at S phase and G2/M phase revealing that CDK2 could be the plausible biological target. Thus, the most cytotoxic candidates
5c
and
8a
were evaluated
in vitro
for their CDK2 inhibitory activity and were able to display significant inhibitory action. The molecular docking study confirmed the obtained results. ADME study predicted that
5c
had appropriate drug-likeness properties. These findings highlight a rationale for further development and optimisation of novel CDK2 inhibitors.
Eight new mixed ligands metal complexes have been prepared by the reaction of Fe(II), Co(II), Ni(II) and Cu(II) with (1:1:1 molar ratio) of ciprofloxacin -eugenol or levofloxacin -eugenol mixed ligands in alkaline medium. The coordination of the mixed ligands toward metal ions has been anticipated in the light of elemental analysis, molar conductance, spectral infrared (IR), ultraviolet-visible (UV-Vis) and magnetic measurements were bidentate ligands. Electronic and magnetic data suggested the octahedral configuration for all these new complexes. The molar conductance data for the metal complexes show nonelectrolytic behaviour in DMF solvent and non-electrolytic properties, also they were no conducting electrical current. The biological activity of the prepared complexes was studied with positive and negative Gram-positive bacteria and good antibacterial results.
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