The application of isatin-based multicomponent-reactions in the quest for new bioactive and druglike molecules

Brandão, Pedro; Marques, Carolina S.; Burke, Anthony J.; Piñeiro, Marta

doi:10.1016/j.ejmech.2020.113102

Cited by 97 publications

(41 citation statements)

References 162 publications

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“…SwissADME is a freely available tool in silico to evaluate compounds’ druglike properties, including absorption, distribution, metabolism, and excretion, using some predictive rules applied by pharmaceutical chemists ( Daina et al, 2017 ; Brandao et al, 2021 ). Parameters such as Veber Lipinski and bioavailability can be calculated.…”

Section: Resultsmentioning

confidence: 99%

Identification of a Novel Ferroptosis Inducer for Gastric Cancer Treatment Using Drug Repurposing Strategy

Zhang

Gao

Niu

et al. 2022

Front. Mol. Biosci.

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Gastric cancer remains one of the major contributors to global cancer mortality, although there is no promising target drug in clinics. Hence, the identification of novel targeted drugs for gastric cancer is urgent. As a promising strategy for inducing ferroptosis for gastric cancer treatment, the ferroptosis inducer is a potential drug. Nevertheless, no ferroptosis inducer has entered clinics. So, our purpose was to identify a novel ferroptosis inducer for gastric cancer treatment using a drug repurposing strategy. Firstly, using a drug repurposing strategy with the aid of a commercialized compound library, HC-056456, a small molecule bioactive CatSper channel blocker, was characterized to inhibit the growth of gastric cancer line MGC-803. At the same time, this anti-proliferation effect can be blocked by ferrostatin-1, a ferroptosis inhibitor, indicating that HC-056456 is a ferroptosis inducer. Then, HC-056456 was identified to decrease GSH content via p53/SLC7A11 signaling pathway. Then Fe2+ and lipid peroxide were accumulated when cells were exposed to HC-056456. Finally, HC-056456 was found to suppress the growth of gastric cancer cells by increasing p53 and repressing SLC7A11 in vivo but not in the presence of ferrostatin-1. In sum, we systematically elucidate that HC-056456 exerts anti-gastric cancer effect by provoking ferroptosis in vitro and in vivo, suggesting its potential role in gastric cancer treatment.

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Section: Resultsmentioning

confidence: 99%

Identification of a Novel Ferroptosis Inducer for Gastric Cancer Treatment Using Drug Repurposing Strategy

Zhang

Gao

Niu

et al. 2022

Front. Mol. Biosci.

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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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“…Schiff are reported to exhibit broad-spectrum chemotherapeutic properties such as antifungal, antimicrobial, antiulcer, antibiot-Synthesis, Antimicrobial Evaluation of Substituted Indole and Nitrobenzenamine based Cr(III), Mn(III) and Fe(III) Metal Complexes ic, antioxidant, antibacterial, anticancer, antimalarial anti-inflammatory, analgesic [7], Anti-oxidative, antimicrobial [8], anti-tubercular [9], Antiepileptic [10], antiviral [11], anticonvulsant [12], antiprotozoal [13] and anti-HIV [14] activities. In the present work authors report the characterization and antimicrobial evaluation of newly synthesized Schiff base metal complexes derived from substituted indole and 4-nitrobenzenamine.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Antimicrobial Evaluation of Substituted Indole and Nitrobenzenamine based Cr(III), Mn(III) and Fe(III) Metal Complexes

2021

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Schiff base ligand (E)-5-methyl-3-(1-(4-nitrophenylimino)ethyl)-1H-indol-2-amine was synthesized by the condensation of 1-(2-amino-5-methyl-1H-indol-3-yl)ethanone and 4-nitrobenzenamine in methanol at 70 oC. The prepared Schiff base ligand doped with Cr(III), Mn(III) and Fe(III) ion, respectively and it is denoted as [M(C34H32N8O4)X]X2. The complexes have been characterized with the help of elemental analysis, conductance measurements, magnetic measurements and their structural configuration have been determined by various spectroscopic (electronic, IR, 1H NMR, 13C NMR, GCMS) techniques. Electronic and magnetic moments of the complexes indicate that the geometry of the metal center was five coordinate square pyramidal. These metal complexes were also tested for their antimicrobial activities to assess their inhibiting potential against Staphylococcus aureus, Bacillus subtilis (positive bacteria) and Pseudomonas aeruginosa, Escherichia coli, Salmonella typhi (negative bacteria) and fungi Rizoctonia sp., Aspergillus sp., Penicillium sp. [Cr(C34H32N8O4)OAc](OAc)2 shows best antimicrobial activity against all the pathogens.

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The application of isatin-based multicomponent-reactions in the quest for new bioactive and druglike molecules

Cited by 97 publications

References 162 publications

Identification of a Novel Ferroptosis Inducer for Gastric Cancer Treatment Using Drug Repurposing Strategy

Identification of a Novel Ferroptosis Inducer for Gastric Cancer Treatment Using Drug Repurposing Strategy

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

Synthesis, Antimicrobial Evaluation of Substituted Indole and Nitrobenzenamine based Cr(III), Mn(III) and Fe(III) Metal Complexes

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