2-Substituted-3-(5-Substituted-1,3,4-oxadiazol/thiadiazol-2-yl) Thiazolidin-4-one Derivatives: Synthesis, Anticancer, Antimicrobial, and Antioxidant Potential

Kumar, Davinder; Aggarwal, Navidha; Kumar, Harsh; Kapoor, Garima; Deep, Aakash; Bibi, Shabana; Sharma, Aastha; Chopra, Hitesh; Marwaha, Rakesh Kumar; Alshammari, Abdulrahman; Alharbi, Metab; Hayee, Abdul

doi:10.3390/ph16060805

Cited by 6 publications

(1 citation statement)

References 33 publications

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“…For these reasons, antitumor antibiotics are amongst the most important of the cancer chemotherapeutic agents [53]. Among novel chemical entities in preclinical studies, in turn, the potential role of TZD-based compounds for future dual antimicrobial and anticancer applications has already been pointed out by other researchers [53][54][55][56][57].…”

Section: Rationalementioning

confidence: 99%

Combined In Silico and In Vitro Analyses to Assess the Anticancer Potential of Thiazolidinedione–Thiosemicarbazone Hybrid Molecules

Paneth,

Kaproń,

Plech

et al. 2023

IJMS

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The number of people affected by cancer and antibiotic-resistant bacterial infections has increased, such that both diseases are already seen as current and future leading causes of death globally. To address this issue, based on a combined in silico and in vitro approach, we explored the anticancer potential of known antibacterials with a thiazolidinedione–thiosemicarbazone (TZD–TSC) core structure. A cytotoxicity assessment showed encouraging results for compounds 2–4, with IC50 values against T98G and HepG2 cells in the low micromolar range. TZD–TSC 3 proved to be most toxic to cancer cell lines, with IC50 values of 2.97 ± 0.39 µM against human hepatoma HepG2 cells and IC50 values of 28.34 ± 2.21 µM against human glioblastoma T98G cells. Additionally, compound 3 induced apoptosis and showed no specific hemolytic activity. Furthermore, treatment using 3 on cancer cell lines alters these cells’ morphology and further suppresses migratory activity. Molecular docking, in turn, suggests that 3 would have the capacity to simultaneously target HDACs and PPARγ, by the activation of PPARγ and the inhibition of both HDAC4 and HDAC8. Thus, the promising preliminary results obtained with TZD–TSC 3 represent an encouraging starting point for the rational design of novel chemotherapeutics with dual antibacterial and anticancer activities.

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Section: Rationalementioning

confidence: 99%

Combined In Silico and In Vitro Analyses to Assess the Anticancer Potential of Thiazolidinedione–Thiosemicarbazone Hybrid Molecules

Paneth,

Kaproń,

Plech

et al. 2023

IJMS

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Synthesis, characterization, antimicrobial and antioxidant activity of 2- (2′-hydroxyphenyl) -1,3,4-oxadiazolyl-5-amino acid derivatives

Souad Abbassi,

Lahreche,

Briki

et al. 2024

Journal of Saudi Chemical Society

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Synthesis, Characterization, Biological Assay of New 5-(Pyridine-2-Yl)-1,3,4-Oxadiazol-2-Amine Derivatives and their Molecular Docking Studies

Madhukar,

Domala

2024

Orient. J. Chem

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This study introduces a novel class of titled compounds, that are produced through a reaction of picolinohydrazide with various unsymmetrical anhydrides. The confirmation of the successful syntheses is affirmed through a detailed characterization protocol including Proton-NMR, 13C-NMR, FTIR, and Mass spectral studies. The resulting products, 2 as well as 3(a-e), underwent successive evaluations to determine their antibacterial capabilities on S. aureus and E. coli, and antifungal evaluation in relation to Candida albicans. Assessment of antimicrobial activity using the disc diffusion method and reference compounds revealed good efficacy in most of these synthesized compounds, revealing some that had very approving results. Computational docking showed that all new compounds exhibit good interactions. This study highlights the power of 5-(pyridine-2-yl)-1,3,4-oxadiazolo alkanamides against both anti-microbial strains.

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2-Substituted-3-(5-Substituted-1,3,4-oxadiazol/thiadiazol-2-yl) Thiazolidin-4-one Derivatives: Synthesis, Anticancer, Antimicrobial, and Antioxidant Potential

Cited by 6 publications

References 33 publications

Combined In Silico and In Vitro Analyses to Assess the Anticancer Potential of Thiazolidinedione–Thiosemicarbazone Hybrid Molecules

Combined In Silico and In Vitro Analyses to Assess the Anticancer Potential of Thiazolidinedione–Thiosemicarbazone Hybrid Molecules

Synthesis, characterization, antimicrobial and antioxidant activity of 2- (2′-hydroxyphenyl) -1,3,4-oxadiazolyl-5-amino acid derivatives

Synthesis, Characterization, Biological Assay of New 5-(Pyridine-2-Yl)-1,3,4-Oxadiazol-2-Amine Derivatives and their Molecular Docking Studies

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