Exploration of Antioxidant, Anti-inflammatory and Anticancer Potential of Substituted 4-Thiazolidinone Derivatives: Synthesis, Biological Evaluation and Docking Studies

Archna,; Chawla, Pooja; Teli, Ghanshyam; Pathania, Shelly; Singh, Shamsher; Srivastava, Vandana

doi:10.1080/10406638.2021.2019796

Cited by 14 publications

(2 citation statements)

References 39 publications

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“…Some of the N‐heterocyclic containing EGFR inhibitor approved by the US FDA are shown in Figure 5 [44,59] . Moreover, N‐heterocyclic compounds exhibit different biological properties such as anti‐HIV, antidiabetic, herbicidal activity, anticancer activity, insecticidal agents, anti‐inflammatory, [60] antibacterial, [41b] antioxidant, [44,61] anticonvulsant, [58b,62] antiallergic, and enzyme inhibitors. These N‐heterocyclic rings also meet the fundamental pharmacophore which is a prerequisite requirement for any molecule to be an EGFR inhibitor.…”

Section: Importance Of Nitrogen Containing Heterocyclic Compound As E...mentioning

confidence: 99%

Nitrogen‐Containing Heterocyclic Scaffolds as EGFR Inhibitors: Design Approaches, Molecular Docking, and Structure‐Activity Relationships

Pal¹,

Teli²,

Matada³

et al. 2023

ChemistrySelect

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proved to be the magical weapon in designed and discovery of synthetic molecules as they acquired comprehensive range of pharmacological properties. In recent year (2018-2022) Nheterocyclic derivatives were uncovered as the potential EGFR TKIs. The present review summarised the research progress of EGFR TKIs to dazed the limitations of currently accessible drugs by consecrating, anatomy, mutation of EGFR, and its role in different types of cancer. The review highlights the medicinal chemistry prospective emphasising about the designing strategies, docking studies, biological evaluation, selectivity and structural activity relationship of N-heterocyclic compounds. Our review will support the medicinal chemists in direction for the development of novel N-heterocyclic based EGFR TKIs.

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Section: Importance Of Nitrogen Containing Heterocyclic Compound As E...mentioning

confidence: 99%

Nitrogen‐Containing Heterocyclic Scaffolds as EGFR Inhibitors: Design Approaches, Molecular Docking, and Structure‐Activity Relationships

Pal¹,

Teli²,

Matada³

et al. 2023

ChemistrySelect

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“…[22,23] In recent times, a promising avenue of investigation has arisen, that focuses on 4-thiazolidinone derivatives as antimitotic agents. [24,25] These molecules have demonstrated efficacy against diverse cancer cell lines, melanoma, lung, colon, ovarian, renal, prostate, and breast cancers, in addition to interacting with various other anticancer agents as shown in Figure 1. [26] Another promising avenue for the creation of novel and efficacious cytotoxic agents lies in the 1,2,3-triazole ring system (10-13).…”

Section: Introductionmentioning

confidence: 99%

Oxindoline Containing Thiazolidine‐4‐one Tethered Triazoles Act as Antimitotic Agents by Targeting Microtubule Dynamics

Shahjahan,

Naraharisetti,

Begum

et al. 2024

ChemistrySelect

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Oxindoline containing thiazolidine‐4‐ones linked triazole hybrids (24 a–l) series were synthesized by multistep synthesis and tested for their cytotoxic activity against four human cancer cell lines. Significantly higher susceptibility was observed in liver (HepG2) cancer cells. Among them conjugates 24 c and 24 e exhibited promising cytotoxicity with IC50 values of 1.64 μM, and 2.07 μM respectively when compared to the standard 5‐fluorouracil (IC50=20.8 μM) against the HepG2 cell line. Later on, these compounds changed the morphology of HepG2 cells and significantly inhibited colony formation in HepG2 in a dose‐dependent manner. The scratch assay divulged that these compounds decreased wound size and inhibited cell migration. Interestingly, they induced the cell cycle arrest at the S phase. Moreover, the DCFDA assay indicated ROS production proportionate to compound dose and AO/Eb staining revealed increased apoptotic cell count with higher doses. The tubulin polymerization assay reveals that they inhibited the microtubules and acted as antimitotic agents. In‐silico results of these conjugates also support their tubulin inhibitory properties. Interestingly, these compounds have adequate ADME‐toxicity parameters. Based on free energy calculation results, it was observed that these inhibitors influence the conformational flexibility of the target tubulin protein.

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An updated literature on BRAF inhibitors (2018–2023)

Maji¹,

Teli²,

Raghavendra

et al. 2023

Mol Divers

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Exploration of Antioxidant, Anti-inflammatory and Anticancer Potential of Substituted 4-Thiazolidinone Derivatives: Synthesis, Biological Evaluation and Docking Studies

Cited by 14 publications

References 39 publications

Nitrogen‐Containing Heterocyclic Scaffolds as EGFR Inhibitors: Design Approaches, Molecular Docking, and Structure‐Activity Relationships

Nitrogen‐Containing Heterocyclic Scaffolds as EGFR Inhibitors: Design Approaches, Molecular Docking, and Structure‐Activity Relationships

Oxindoline Containing Thiazolidine‐4‐one Tethered Triazoles Act as Antimitotic Agents by Targeting Microtubule Dynamics

An updated literature on BRAF inhibitors (2018–2023)

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