Evaluation of novel synthesized thiazole derivatives as potential aromatase inhibitors against breast cancer.
Eman FayadDalal Nasser BinjawharAbeer A AgeeliDalal Sulaiman AlshayaFahmy Gad ElsaidAmr Yasser MahmoudEman M RadwanMohamed Ahmed Elian SophyAhmed Re MahdyPublished in: Future medicinal chemistry (2024)
Background: 4-Methylacetophenone is used in the preparation of starting materials, 4-methylphenacyle bromide ( 2 ) and 4-methylacetophenone thiosemicarbazole ( 3 ). Results: Several novel 2,4-disubstituted-1,3-thiazole analogues were obtained via the treatment of starting materials with 4-methylphenacyl bromide, acetyl chloride, aromatic aldehydes and bromination providing thiazole derivatives 5-8 respectively. Conclusion: Compounds 5-8 were investigated for their cytotoxic activity on MCF-7 and normal breast cells. Active compounds were found and in contrast to staurosporine, compound 8 displayed the most potent cytotoxic action that showed a strong inhibitory effect (aromatase) and (protein tyrosine kinase) enzymes, proving that the novel thiazole derivatives promoted the effective anticancer drug candidates.
Keyphrases
- tyrosine kinase
- epidermal growth factor receptor
- induced apoptosis
- structure activity relationship
- magnetic resonance
- amino acid
- cell cycle arrest
- breast cancer cells
- molecular docking
- endoplasmic reticulum stress
- magnetic resonance imaging
- cell proliferation
- oxidative stress
- emergency department
- atomic force microscopy
- mass spectrometry
- combination therapy
- small molecule
- human health
- signaling pathway
- anti inflammatory
- replacement therapy