Isatin, 1H-indole-2,3-dione, is a heterocyclic compound of significant importance in medicinal chemistry. It is a synthetically versatile molecule, a precursor for a large number of pharmacologically active compounds. Isatin and its derivatives have aroused great attention in recent years due to their wide variety of biological activities, relevant to application as insecticides and fungicides and in a broad range of drug therapies, including anticancer drugs, antibiotics and antidepressants. The purpose of this review is to provide an overview of the pharmacological activities of isatin and its synthetic and natural derivatives. Molecular modifications to tailor the properties of isatin and its derivatives are also discussed.

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The present study investigates the binding interaction between a water-soluble Schiff base, N,N'-bis{5-[(triphenylphosphonium chloride)-methyl]salicylidine}-o-phenylenediamine (SF), and calf thymus DNA (CT-DNA) using emission, absorption, circular dichroism, and viscosity studies. In fluorimetric studies, the dynamic enhancement constant (K(D)) and bimolecular enhancement constant (K(B)) were calculated at different temperatures and demonstrated that fluorescence enhancement is not initiated by a dynamic process, but instead by a static process that involves complex DNA formation in the ground state. Further, the enthalpy and entropy of the reaction between SF and CT-DNA showed that the reaction is exothermic and enthalpy-favored (DeltaH = -153.51 kJ mol(-1); DeltaS = -427.67 J mol(-1) K). In addition, detectable changes in the circular dichroism spectrum of CT-DNA in the presence of SF indicated deep conformational changes in the DNA double helix following interaction with SF. Further, the Schiff base at different concentrations is able to perform cleavage of pUC18 plasmid DNA. All these results prove that SF interacts with CT-DNA via an intercalative mode of binding.