Isatin dimers and their biological activities

Zhang, Yazhou; Liu, Hai‐Lin; He, Qing; Xu, Zhi

doi:10.1002/ardp.201900299

Cited by 47 publications

(12 citation statements)

References 90 publications

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“…Although a number of reviews on the synthesis and biological applications of isatins have recently appeared [ 8 , 9 ], the current review’s goal is to keep readers up to date on the biological applications of isatin derivatives and isatin hybrids, with a focus on cancer and Neglected Tropical Diseases such as malaria, tuberculosis, bacterial infections, and parasitic diseases.…”

Section: Introductionmentioning

confidence: 99%

A Mini Review on Isatin, an Anticancer Scaffold with Potential Activities against Neglected Tropical Diseases (NTDs)

et al. 2022

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Isatin, chemically an indole-1H-2,3-dione, is recognised as one of the most attractive therapeutic fragments in drug design and development. The template has turned out to be exceptionally useful for developing new anticancer scaffolds, as evidenced by the increasing number of isatin-based molecules which are either in clinical use or in trials. Apart from its promising antiproliferative properties, isatin has shown potential in treating Neglected Tropical Diseases (NTDs) not only as a parent core, but also by attenuating the activities of various pharmacophores. The objective of this mini-review is to keep readers up to date on the latest developments in the biological potential of isatin-based scaffolds, targeting cancer and NTDs such as tuberculosis, malaria, and microbial infections.

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Section: Introductionmentioning

confidence: 99%

A Mini Review on Isatin, an Anticancer Scaffold with Potential Activities against Neglected Tropical Diseases (NTDs)

et al. 2022

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“…As a representative of the class of privileged structures, isatin and its derivatives are widely used in medicinal chemistry [1,2]. The progressing number of works on synthetic procedures [3] and the studies of this heterocycle push researchers in this area to publish generalized data on one or another type of biological activity [4][5][6][7]. It is due to the manifestation of isatin and its derivatives of a wide spectrum of activity, such as anti-cancer [8][9][10], anti-tubercular [11,12], antibacterial [13], anti-COVID [14,15], fungicidal [16,17], etc (Fig.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and diverse biological activity profile of triethylammonium isatin-3-hydrazones

Богданов¹,

Tsivileva²,

Voloshina³

et al. 2022

ADMET DMPK

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A series of biorelevant triethylammonium isatin hydrazones containing various substituents in the aromatic fragment have been synthesized. Their structure and composition were confirmed by NMR- and IR-spectroscopies, mass-spectrometry and elemental analysis. It was found that some representatives show activity against Staphylococcus aureus and Bacillus cereus higher or at the level of norfloxacin, including methicillin-resistant Staphylococcus aureus strains. The study also showed low hemo- and cytotoxicity (Chang Liver) and high antiaggregatory and anticoagulant activity of these compounds. The high potential of new ammonium isatin-3-acylhydrazones in the search for antimicrobial activity against phytopathogens of bacterial and fungal nature has been shown for the first time.

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“…Being a member of the ‘privileged structure’ class, the isatin heterocyclic platform is widely used in pharmaceutical chemistry [10,11] Numerous studies have shown that derivatives of this heterocycle exhibit various types of biological activity, such as antiviral, antifungal, antibacterial, antiproliferative, antitumor, etc [12–19] . However, the usually low solubility of these compounds in biocompatible solvents does not allow more detailed studies of other types of their activity.…”

Section: Introductionmentioning

confidence: 99%

Isatin‐3‐acylhydrazones with Enhanced Lipophilicity: Synthesis, Antimicrobial Activity Evaluation and the Influence on Hemostasis System

Богданов

Voloshina

Sapunova

et al. 2022

Chemistry & Biodiversity

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Water‐soluble trialkylammonium isatin‐3‐hydrazone derivatives bearing phenolic substituent were easily synthesized with high yields. XRD studies confirmed the presence of these compounds as trans‐(Z)‐isomers in a crystal. It was shown that an increase in the lipophilicity of the cationic center leads to an increase in activity against Gram‐positive bacteria Staphylococcus aureus and Bacillus cereus, including methicillin‐resistant Staphylococcus aureus (MRSA) strains. The MIC values of all compounds turned out to be 2–100 times higher than the MIC of norfloxacin against the MRSA strains in the absence of hemo‐ and cytotoxicity. Antiaggregation and anticoagulation properties were in vitro better than for acetylsalicylic acid and sodium heparin drugs. It has been shown by UV spectroscopy and fluorescence microscopy that the mechanism of antimicrobial action of new acylhydrazones is associated with their ability to destroy the bacterial cell membrane.

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Isatin dimers and their biological activities

Cited by 47 publications

References 90 publications

A Mini Review on Isatin, an Anticancer Scaffold with Potential Activities against Neglected Tropical Diseases (NTDs)

A Mini Review on Isatin, an Anticancer Scaffold with Potential Activities against Neglected Tropical Diseases (NTDs)

Synthesis and diverse biological activity profile of triethylammonium isatin-3-hydrazones

Isatin‐3‐acylhydrazones with Enhanced Lipophilicity: Synthesis, Antimicrobial Activity Evaluation and the Influence on Hemostasis System

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