Novel Thiazole Substituted Imidazolin-5-ones: Synthesis, Biological Screening and Molecular Docking Studies

It has been suggested that sphingosine kinase 1 (3VZD) is essential for the advancement of cancer. Increased expression of SK1 mRNA transcript and/or SK1 protein has been seen in cases of non-Hodgkin lymphoma and malignancies of the stomach, lung, brain, colon, kidney, and breast. Patients with oestrogen receptor (ER)-positive breast cancer have also been found to induce tamoxifen resistance, and high tumour expression of SK1 is associated with poor patient survival rates. As a result, medications that block or decrease 3VZD may have antibacterial and anticancer effects. A series of eleven imidazolin-5-ones substituted with thiazoles were synthesised and their antibacterial, antioxidant, and anticancer properties assessed. Moreover, molecular docking experiments on the 3VZD target protein were carried out to confirm our theory. IMD5 and IMD7 were shown to be the most effective drugs against the MDA MB 231 (Triple Negative Breast Cancer) cell line in in vitro anticancer experiments. IMD11 was shown to be active when antioxidant activity was assessed using the DPPH free radical scavenging technique. Using the microorganisms B. subtilis, S. aureus, E. coli, and P. aeruginosa, antibacterial activity was investigated. It was discovered that IMD9, IMD10, and IMD11 were active against Pseudomonas aeruginosa NCIM-5029, whereas IMD4 and IMD5 had action against Candida albicans.

Publication Details

Journal
Zenodo (CERN European Organization for Nuclear Research)
Published
2025-06-07
DOI
https://doi.org/10.5281/zenodo.15614904
Primary Topic
Sphingolipid Metabolism and Signaling
Type
article
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article

Novel Thiazole Substituted Imidazolin-5-ones: Synthesis, Biological Screening and Molecular Docking Studies

Zenodo (CERN European Organization for Nuclear Research)
Sphingolipid Metabolism and Signaling
article

Novel Thiazole Substituted Imidazolin-5-ones: Synthesis, Biological Screening and Molecular Docking Studies

article en

Abstract

It has been suggested that sphingosine kinase 1 (3VZD) is essential for the advancement of cancer. Increased expression of SK1 mRNA transcript and/or SK1 protein has been seen in cases of non-Hodgkin lymphoma and malignancies of the stomach, lung, brain, colon, kidney, and breast. Patients with oestrogen receptor (ER)-positive breast cancer have also been found to induce tamoxifen resistance, and high tumour expression of SK1 is associated with poor patient survival rates. As a result, medications that block or decrease 3VZD may have antibacterial and anticancer effects. A series of eleven imidazolin-5-ones substituted with thiazoles were synthesised and their antibacterial, antioxidant, and anticancer properties assessed. Moreover, molecular docking experiments on the 3VZD target protein were carried out to confirm our theory. IMD5 and IMD7 were shown to be the most effective drugs against the MDA MB 231 (Triple Negative Breast Cancer) cell line in in vitro anticancer experiments. IMD11 was shown to be active when antioxidant activity was assessed using the DPPH free radical scavenging technique. Using the microorganisms B. subtilis, S. aureus, E. coli, and P. aeruginosa, antibacterial activity was investigated. It was discovered that IMD9, IMD10, and IMD11 were active against Pseudomonas aeruginosa NCIM-5029, whereas IMD4 and IMD5 had action against Candida albicans.

Zenodo (CERN European Organization for Nuclear Research)
Good health and well-being
Openalex Percentile: Top 60%
Sphingolipid Metabolism and Signaling
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Novel Thiazole Substituted Imidazolin-5-ones: Synthesis, Biological Screening and Molecular Docking Studies · Zenodo (CERN European Organization for Nuclear Research) (2025) | TGRS Research Map | TGRS