Therapeutic Outcomes of Isatin and Its Derivatives against Multiple Diseases: Recent Developments in Drug Discovery

Abstract

Isatin (1H indole 2, 3-dione) is a heterocyclic, endogenous lead molecule recognized in humans and different plants. The isatin nucleus and its derivatives are owed the attention of researchers due to their diverse pharmacological activities such as anticancer, anti-TB, antifungal, antimicrobial, antioxidant, anti-inflammatory, anticonvulsant, anti-HIV, and so on. Many research chemists take advantage of the gentle structure of isatins, such as NH at position 1 and carbonyl functions at positions 2 and 3, for designing biologically active analogues via different approaches. Literature surveys based on reported preclinical, clinical, and patented details confirm the multitarget profile of isatin analogues and thus their importance in the field of medicinal chemistry as a potent chemotherapeutic agent. This review represents the recent development of isatin analogues possessing potential pharmacological action in the years 2016–2020. The structure–activity relationship is also discussed to provide a pharmacophoric pattern that may contribute in the future to the design and synthesis of potent and less toxic therapeutics.

Exploring novel derivatives of isatin-based Schiff bases as multi-target agents: design, synthesis,in vitrobiological evaluation, andin silicoADMET analysis with molecular modeling simulations

“…[17][18][19][20][21][22] In recent decades, the isatin (2,3-dioxindole) (I) molecule has attracted the concern of scientists for its potent biological and therapeutic applications. [23][24][25] Also, isatin derivatives have numerous distinct biological activities. Ethyl 4-chlorobenzoyl hydrazono-2-oxoindolin-1-yl acetate II is biologically active as a powerful in vitro inhibitor for an a-amylase enzyme (antidiabetic agent).…”

Glyco-conjugated thiosemicarbazones of substituted isatin containing D-galactose moiety: Synthesis, bacterial/fungal inhibition assay and molecular docking study

“…On the other hand, isatin (1H-Indole-2,3-dione) contains two reactive functional groups, including the amide and the ketone. It has been found that isatin itself does not exhibit any biological activity, but the derivatives containing this ring exhibit many interesting biological activities [7]. Many such compounds have been used as drugs in the treatment of human diseases, such indirubin, methisazone, NSC73306, semaxanib [8], sunitinib [9], and toceranib [10] (Fig.…”

1-Benzyl-5-bromo-3-hydrazonoindolin-2-ones as Novel Anticancer Agents: Synthesis, Biological Evaluation and Molecular Modeling Insights

“…The isatin motif has surfaced as a privileged scaffold with numerous and significant pharmacological actions [ 13 ], such as antimicrobial [ 14 ], antiviral [ 15 ], and anticancer [ 16 ] effects. Noteworthy, isatin moiety has been included in some clinically approved medications such as Nintedanib and Sunitinib ( Figure 1 ).…”