Anticancer Potential of Compounds Bearing Thiazolidin-4-one Scaffold: Comprehensive Review

Singh, Dalbir; Piplani, Mona; Kharkwal, Harsha; Murugesan, Sankaranarayanan; Singh, Yogendra; Aggarwal, Amit; Chander, Subhash

doi:10.51847/ohzuia1yg6

Cited by 4 publications

(1 citation statement)

References 81 publications

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“…[7] According to reports, the heterocyclic thiazolidine-2,4-dione (TZD) compounds may typify as a critical scaffold in the remedy of cancer. TZDs were announced to express antitumor practice in an expansive assortment of investigational cancer models via amending the cell turn, inducing necroptosis and cell distinctiveness over and above by constraining tumefaction angiogenesis [8][9][10] which is considered as a weighty basis for the enlargement and excrescence of malicious mass. [11] According to studies, a number of TZD compounds, such as ciglitazone (I), are effective anticancer agents and angiogenesis inhibitors that target VEGFR-2 by reducing VEGF synthesis in an in vitro model.…”

Section: Introductionmentioning

confidence: 99%

Design, synthesis, and docking of novel thiazolidine‐2,4‐dione multitarget scaffold as new approach for cancer treatment

Hanafy

El‐Hddad

Abdelgawad

et al. 2023

Archiv der Pharmazie

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Novel thiazolidine‐2,4‐diones have been developed and estimated as conjoint inhibitors of EGFRT790M and VEGFR‐2 against HCT‐116, MCF‐7, A549, and HepG2 cells. Compounds 6a, 6b, and 6c were known to be the dominant advantageous congeners against HCT116 (IC50 = 15.22, 8.65, and 8.80 µM), A549 (IC50 = 7.10, 6.55, and 8.11 µM), MCF‐7 (IC50 = 14.56, 6.65, and 7.09 µM) and HepG2 (IC50 = 11.90, 5.35, and 5.60 µM) mass cell lines, correspondingly. Although compounds 6a, 6b, and 6c disclosed poorer effects than sorafenib (IC50 = 4.00, 4.04, 5.58, and 5.05 µM) against the tested cell sets, congeners 6b and 6c demonstrated higher actions than erlotinib (IC50 = 7.73, 5.49, 8.20, and 13.91 µM) against HCT116, MCF‐7 and HepG2 cells, yet lesser performance on A549 cells. The hugely effective derivatives 4e–i and 6a–c were inspected versus VERO normal cell strains. Compounds 6b, 6c, 6a, and 4i were found to be the most effective derivatives, which suppressed VEGFR‐2 by IC50 = 0.85, 0.90, 1.50, and 1.80 µM, respectively. Moreover, compounds 6b, 6a, 6c, and 6i could interfere with the EGFRT790M performing strongest effects with IC50 = 0.30, 0.35, 0.50, and 1.00 µM, respectively. What is more, 6a, 6b, and 6c represented satisfactory in silico computed ADMET profile.

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Section: Introductionmentioning

confidence: 99%

Design, synthesis, and docking of novel thiazolidine‐2,4‐dione multitarget scaffold as new approach for cancer treatment

Hanafy

El‐Hddad

Abdelgawad

et al. 2023

Archiv der Pharmazie

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Design, Synthesis, Anticancer and Antimicrobial Studies of 2‐Phenylthiazolidin‐4‐one Glycinamide Conjugates

Singh,

Aggarwal,

Patel

et al. 2023

ChemistrySelect

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Thiazolidin‐4‐one is a versatile nucleus that has been reported to exhibit a diverse array of biological activities, including anticancer and antimicrobial activities. In the current research study, a series of C2‐(p‐substituted phenyl)‐thiazolidin‐4‐one compounds conjugated with anilines were designed and tested for drug‐likeness behaviour. Subsequently, the designed compounds were synthesized, characterized, and tested for anticancer activity against three cancer cell lines, namely liver (HEP−G2 cells), breast (MDA‐MB‐231), and glioblastoma (U87MG cells), with gemcitabine as the reference positive control drug. Initially, the compounds were tested at 50 micromolar, while the MIC was determined for the selected active compounds. Among the three cell lines, MDA‐MB‐231 showed relatively higher sensitivity towards the tested compounds. Four compounds of the series exhibited comparable or superior cytotoxicity to the reference drug gemcitabine. Particularly, N‐(p‐tolyl)‐2‐(2‐(4‐methoxyphenyl)‐4‐oxothiazolidin‐3‐yl)acetamide (6 d) displayed highest cytotoxicity among the series. The anticancer activity of the selected compounds was also tested against 3D spheroid models, in which compound N‐(4‐chlorophenyl)‐2‐(2‐(4‐methoxyphenyl)‐4‐oxothiazolidin‐3‐yl)acetamide (6 a) induced apoptosis in brain tumour spheroids (MTS). Docking studies of compound 6 d were performed against different targets, namely dihydrofolate reductase, phosphoinositide 3‐kinase, epidermal growth factor receptor, dihydroorotate dehydrogenase, and murine double minute 2, which illustrated inhibition of dihydroorotate dehydrogenase as a possible mechanism of toxicity. The compounds were also evaluated in vitro for antibacterial activity against two bacterial strains (E. coli and P. aeruginosa) and a Candida albicans fungal strain.

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Bioimaging of thiazolidine-4-one-based new probes, fluorimetric detection of Cu2+ “on-off” sensor property, DFT calculation, molecular docking studies, and multiple real samples application

Karakiliç,

Başçeken,

Eskiler

et al. 2025

Food Chemistry

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Anticancer Potential of Compounds Bearing Thiazolidin-4-one Scaffold: Comprehensive Review

Cited by 4 publications

References 81 publications

Design, synthesis, and docking of novel thiazolidine‐2,4‐dione multitarget scaffold as new approach for cancer treatment

Design, synthesis, and docking of novel thiazolidine‐2,4‐dione multitarget scaffold as new approach for cancer treatment

Design, Synthesis, Anticancer and Antimicrobial Studies of 2‐Phenylthiazolidin‐4‐one Glycinamide Conjugates

Bioimaging of thiazolidine-4-one-based new probes, fluorimetric detection of Cu2+ “on-off” sensor property, DFT calculation, molecular docking studies, and multiple real samples application

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