Isatin: A Scaffold with Immense Biodiversity

Abstract

: Isatin is an endogenous and a significant category of fused heterocyclic component, widely been a part of several potential biologically useful synthetics. Since its discovery, tons of research work has been conducted with respect to the synthesis, chemical properties, and biological and industrial applications. It contains indole nucleus having both lactam and keto moiety which while being a part of a molecular framework exerted several biological effects, viz.; antimicrobial, antitubercular, anticonvulsant, anticancer etc. Isatin derivatives are synthetically significant substrates, which can be utilized for the synthesis of huge diversified chemical entities of which few members emerged to be a drug. The reason for this review is to provide extensive information pertaining to the chemistry and its significance in altering several pathological states of isatin and its derivatives. A Structure Activity Relationships study thus developed through a gamut of scientific information indicates the importance of mostly electron withdrawing groups, halogens, nitro, alkoxy and to a minor extent groups with positive inductive effects, such as methyl at position 1, 5, 6 and 7 of isatin in alleviating several clinical conditions. It is also observed from the survey that the presence of two oxo groups at position 2 and 3 sometimes become insignificant as fusion with a heterocycle at those position resulted in a biologically relevant compound.

Synthesis, Biocidal and Antibiofilm Activities of New Isatin–Quinoline Conjugates against Multidrug-Resistant Bacterial Pathogens along with Their In Silico Screening

“…Naturally occurring indole, quinoline and indoloquinoline heterocyclic cores are particularly important due to their diverse biological activities, which inspire many researchers to synthesize series of hybrid systems with different spacers [ 8 , 9 , 10 , 11 ]. Natural and synthetic isatin scaffolds have received much attention from many researchers due to their wide pharmaceutical application as antimicrobial, antioxidant, anticancer and antimalarial agents [ 12 , 13 , 14 , 15 ]. On the other hand, quinoline’s core structure represents a promising surrogate in drug design and development.…”

Design, Synthesis and Anti-Lung Cancer Evaluation of 1, 2, 3-Triazole Tethered Dihydroartemisinin-Isatin Hybrids

“…Isatin derivatives have the potential to act on a variety of drug targets like histone deacetylase, β -carbonic anhydrase, tyrosine kinase and tubulin, and the isatin-based nintedanib has already been approved for the lung cancer therapy ( Sharma et al, 2014 ; Ding et al, 2020 ; Hou et al, 2020 ; Nath et al, 2021 ; Varpe et al, 2021 ). Therefore, isatin derivatives are also considered as useful templates for the development of novel anti-lung cancer agents.…”

Design, synthesis and anti-breast cancer properties of butyric ester tethered dihydroartemisinin-isatin hybrids

“…Isatin, widely distributed in natural kingdom, is a well-known pharmacologically active scaffold [ 17 , 18 ]. Isatin hybrids possessed significant therapeutic effect on breast cancers including drug-resistant forms, good selectivity and low toxic side effects [ 19 , 20 ].…”