Isatin (1H-indole-2,3-dione), an indole derivative of plant origin, is involved in many pharmacological activities like antiallergic, antimalarial, antiviral and antimicrobial; isatin and its derivatives have been found to show promising results against various cancer cell lines. Isatin is a versatile precursor for many biologically active molecules and its diversified nature makes it a versatile substrate for further modifications. This review provides a brief overview on the recent advances and future perspectives on pharmacological aspects of isatin and its derivatives reported in the last decade. Keywords : Isatin, Anticancer, Antimicrobial, Monoamine oxidase, Antiviral

Isatin (indole-2,3-dione) is an endogenous regulator, exhibiting various behavioral, biological, and pharmacological activities. Synthesis of isatin includes several crucial stages: cleavage of the tryptophan side chain and subsequent oxidation of the indole nucleus. Although these stages require concerted action of bacterial and host enzymes, there are two pathways of isatin formation: the host and bacterial pathways. Isatin acts as a neuroprotector in different experimental models of neurodegeneration. Its effects are realized via up- and downregulation of isatin-responsive genes and via interaction with numerous isatin-binding proteins identified in the brain. The effect of isatin on protein-protein interactions in the brain may be important for realization of weak inhibition of multiple receptor targets.

Isatin or 1H-indole-2, 3-dione is an indole derivative. Isatin is an important class of heterocyclic compounds. Recently, heterocyclic compounds analogues and their derivatives have attracted strong interest in medicinal chemistry due to their biological and pharmacological properties. The structure have offered a high value of diversity that is proven useful for the development of new medicinal drugs and improved potency,less toxicity and good pharmacological activity. Isatin has a wide varity of pharmacological activities such as an antimicrobial, anticancer, antiviral, anticonvulsant, anti-inflammatory and analgesic etc. The aim of this review is to provide the recent efforts of scinentists in pharmacological screening of isatin, importants and synthesis of isatin derivatives,pharmacological action of isatin and their biological activity.

Isatin (1H-indolin-2,3-dione) is a versatile bioactive and heterocyclic scaffold with an indole nucleus. For the past decades, isatin and its derivatives have shown tremendous interest among researchers (organic and medicinal chemists). Hence, their extensive structural modification has result in different analogues of isatin depicting wide range of biological and pharmacological activities including antimicrobial, anticancer, anti-inflammatory and analgesic, anticonvulsant, anti-viral, anti HIV and antiplasmodial activity. In this present review, we focus on isatin and its derivatives possessing cytotoxic and anticancer activity against different cancer cell lines from the period 2002 to 2015.

Isatin, also known as 1H-Indole-2, 3-Dione, is an eight-carbon containing endogenous compound found in nature. Erdmann and Laurent synthesized isatin in 1840, before it was discovered in nature. It is versatile and distributed in tissues and body fluids. Isatins have also been detected in mammalian tissue, and their function as a biochemical process modulator has been the focus of many debates. The isatin moiety also shows some important chemical reactions such as oxidation, N-Acylation, Friedel-Crafts reaction, N-Halogenation, etc. Antitumor, antimicrobial, anti-inflammatory, anticonvulsant, antiviral, anti-HIV, antioxidant, and CNS depressant functions are all possessed by simple isatin nucleus. Substituted derivatives of this compound also have these properties. The isatin derivatives are effective inhibitors of the urease and α-glucosidase enzymes. This review provides a brief overview on the some commonly used procedures to synthesize the isatin moiety and its derivatives, its physical properties, reactions and biological activities.

Isatin (1H-indole-2,3-dione) is a chemical found in various medicinal plant species and responsible for a broad spectrum of pharmacological and biological properties that may be beneficial to human health, as an anticonvulsant, antibacterial, antifungal, antiviral, and anticancer agent. The aim of the present study was to determine in vitro the cytotoxic, mutagenic, and apoptotic effects of isatin on CHO-K1 and HeLa cells using the MTT viability assay (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide), micronucleus (MN) test, apoptosis index, and nuclear division index (NDI). The 5 isatin concentrations evaluated in the mutagenicity and apoptosis tests were 0.5, 1, 5, 10, and 50 μM, selected through a preliminary MTT assay. Positive (doxorubicin, DXR) and negative (phosphate buffered saline, PBS) control groups were also included in the analysis. Isatin did not exert a mutagenic effect on CHO-K1 after 3 and 24 h of treatment or on HeLa cells after 24 h. However, 10 and 50 μM concentrations inhibited cell proliferation and promoted apoptosis in both CHO-K1 and HeLa cells. Data indicate that the cytotoxic, apoptotic, and antiproliferative effects of isatin were concentration independent and cell line independent. The authors thank Profa Dra Eiko Nakagawa Itano for the use the spectrophotometer and the Conselho Nacional para o Desenvolvimento Científico e Tecnológico for master's scholarships to P. M. Cândido-Bacani and grants to T. R. Calvo, W. Vilegas, E. A. Varanda and I. M. S. Cólus. The Conselho Nacional para o Desenvolvimento Científico e Tecnológico provided funding for this study.

Isatin (1H-indole-2,3-dione) and its derivatives represent an important class of heterocyclic compounds that can be used as precursors for drug synthesis. Since its discovery, a lot of research work has been done regarding the synthesis, chemical properties, and biological and industrial applications of isatin. In this review, we have reported several novel methods for the synthesis of N-, C2-, and C3-substituted and spiro derivatives of isatin. The isatin moiety also shows important chemical reactions such as oxidation, ring expansion, Friedel-Crafts reaction and aldol condensation. These reactions, in turn, produce several biologically viable compounds like 2-oxindoles, tryptanthrin, indirubins, and many more. We have also summarized some recently reported biological activities exhibited by isatin derivatives, like anti-cancer, anti-bacterial, anti-diabetic and others. Special attention has been paid to their anti-cancer activity, and various anti-cancer targets such as histone deacetylase, carbonic anhydrase, tyrosine kinase, and tubulin have been discussed in detail. Other applications of isatin derivatives, such as in the dye industry and in corrosion prevention, have also been discussed.

Isatin or 1H-indole-2,3-dione or 2,3-dioxindole is an indole derivative. Isatin and its analogs are synthetically useful substances where they may be utilized for the production of a broad range of heterocyclic molecules, which are depicting a wide reach of biological and pharmacological activities, as well as anticancer, anti-inflammatory, antiviral, anticonvulsant, anti-TB, antidiabetic, anti-microbial, antitumor, antimalarial, anti-HIV, antibacterial, anti-analgesic, and antiplasmodial activities. Isatin is a precursor for many synthesized therapeutic molecules that are amenable to pharmacological action and have excellent biological potential. Isatin has a magnificent scaffold for both the natural and synthetic construction of molecules. These molecules are being used in drug therapy such as anticancer, antibiotic, and antidepressant drugs and have many more clinical applications. Due to its privileged scaffolding, the synthetic versatility of isatin has produced many structurally diverse derivatives, including the substitution of mono-, di- and tri- substitution of the aryl rings A and those derived by derivation of isatin nitrogen and C2 and C3 carbon moieties. As a result, improving and expediting access to isatin-related molecules is a challenging study in synthetic organic chemistry.

Isatin (indole-dione-2,3) is an endogenous indole that exhibits a wide spectrum of biological and pharmacological activities. Physiologically relevant concentrations of isatin (ranged from 1 nM to 10 M) did not influence basal activity of soluble human platelet guanylate cyclase (sGC), but caused a bell-shaped inhibition of the NO-activated enzyme. Inhibition of the NO-dependent activation by isatin did not depend on a chemical nature of the NO donors. The inhibitory effects of ODC (a heme-dependent inhibitor of sGC) and isatin were non-additive suggesting that the inhibitory effect of isatin may involve the heme binding domain (possibly heme iron) and experiments with hemin revealed some isatin-dependent changes in its spectrum. Isatin also inhibited sGC activation by the allosteric activator YC-1. It is suggested that the bell shaped inhibition of the NO-dependent activation of sGC by isatin may be attributed to complex interaction of isatin with the heme binding domain and the allosteric YC-1-binding site of sGC.

Isatin (1H-indole-2,3-dione ) and derivatives demonstrate a diverse array of biological activities. Isatin and 5-halo derivatives has reacted to form the schiff’s bases , mannich bases and friedal craft alkylation’s to form C-C, C-N, C=N bonds. From the spectral studies, isatin has undergoes reaction at C-3 and N-1 position and synthesized lead in present schme and seen the similarity of structure and analgesic-anti-inflammatory activity.