Dual activity of indolin-2-ones containing an arylidene motif: DNA and BSA interaction.

Applying a multistep approach, novel indolin-2-ones (IND) that possess an arylidene motif have been synthesized. Eight compounds were chosen for different biological tests (antimicrobial and cytotoxicity). IND containing 2-thienyl (4h) fragment have been found to exhibit good antimicrobial activity against B. cereus . Molecules that have 3-aminophenyl (4d) or 2-pyridyl (4g) groups have shown the best antifungal activities against all tested fungi. These compounds have also been noticed as promising pharmaceuticals against MCF-7 cancer cell lines. Experimental outcomes from the investigation of the interaction of 4d with DNA implied its moderate binding to DNA ( K _SV = 1.35 × 10 ⁴ and 3.05 × 10 ⁴ M ^-1 for EB and Hoechst binder, respectively). However, considerably stronger binding of 4d to BSA has been evidenced ( K _a = 6.1 × 10 ⁶ M ^-1 ). In summary, IND that contains m -aminobenzylidene fragment (4d) exhibits a good dual biological activity making it a promising candidate for further investigation in the drug discovery sector.
Competing Interests: There are no conflicts to declare.
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