Two unsymmetrical oxovanadium complexes incorporating salicylaldehyde derivate and phenanthroline [VO(DESAA)(phen)] (1), (DESAA = 4-(diethylamino)salicylaldehyde anthranilic acid, phen = phenanthroline) and [VO(CLSAA)(phen)] (2), (CLSAA = 5-chlorosalicylaldehyde anthranilic acid)] have been synthesized and characterized. The interactions of the complexes with CT-DNA were studied using different techniques. Complexes 1 and 2 interact with CT-DNA by intercalative modes and can efficiently cleave pBR322 DNA after light irradiation. The two complexes showed high cytotoxic activities against myeloma cell (Ag8.653) and gliomas cell (U251) lines. Interestingly, complex 1 exhibited greater antitumor efficiency, larger binding affinity with CT-DNA, and better cleaving ability than those of complex 2. In addition, their antitumor mechanism has been analyzed by using cell cycle analysis, apoptosis, and Annexin V-FITC/PI assay. The results showed that complex 1 can cause G2/M-phase arrest of the cell cycle, exhibit a significantly induced apoptosis in Ag8.653 cells, and display typical morphological apoptotic characteristics. These complexes induced proliferative suppression of Ag8.653 cells via the induction of apoptosis.

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