Advances in Pharmacology of Isatin and its Derivatives: A Review

Abstract

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.

3′,4′-Dihydro-2′H-spiro[indoline-3,1′-isoquinolin]-2-ones as potential anti-cancer agents: synthesis and preliminary screening

“…Naturally occurring (figure 1) and synthetic OXs have also been found to display a diverse array of biological properties, including antimalarial, antifungal, anticonvulsant, anti-HIV, radical scavenging and antibacterial activities and anti-cancer activities [23][24][25][26][27][28][29]. Their anti-cancer activity is attributed to a number of mechanisms such as inhibition of caspase [30,31], p53 induction [32] and inhibition of the tumour suppressor gene p53 [33].…”

Hybrids of Isatin‐Pyrazole as Potential α‐Glucosidase Inhibitors: Synthesis, Biological Evaluations and Molecular Docking Studies

“…Isatin is an important heterocyclic system because of its inimitable role in medicinal chemistry. Numerous alkaloids, drugs, dyes, pesticides and analytical reagents contain this structural motif in their core structure . A large number of isatin derivatives have been reported in literature exhibiting a wide spectrum of biological activities that include anticancer, antibacterial, antiviral, anticonvulsant, anti‐inflammatory, antifungal activity, etc .…”

“…Numerous alkaloids, drugs, dyes, pesticides and analytical reagents contain this structural motif in their core structure. [13,14] A large number of isatin derivatives have been reported in literature exhibiting a wide spectrum of biological activities that include anticancer, [15] antibacterial, [16] antiviral, [17] anticonvulsant, [18] antiinflammatory, [19] antifungal activity, [20] etc. Isatin derivatives (compound 1-4, Figure 1b) have also been explored for their α-glucosidase inhibitory potential and the results obtained were encouraging.…”

(R*)-1-Benzyl-3-(2-hydroxyphenyl)indoline-2-one

“…It exhibits endogamous activity in mammals (Chaudhary et al, 2013) and has shown cardioinhibitory effects on a frog's heart, and hypotensive, respiratory depression and antidiuretic effects (Pandeya et al, 2005). Isatin also possess anticancer (Khan et al, 2015), antioxidant (Sammaiah & Pragathi, 2014), antiviral (Gomathi et al, 2013), antimicrobial (Saxena et al, 2015), analgesic (Pal et al,201), anti-inflammatory (Hajare & Chinchole, 2013), antitubercular (Aboul-fadl & BinJubair, 2010), anticonvulsant (Raj, 2012) and antianxiety (Grewal, 2014) activities.…”