Evaluation of novel synthesized thiazole derivatives as potential aromatase inhibitors against breast cancer
Eman Fayad, Dalal Nasser Binjawhar, Abeer A Ageeli, Dalal Sulaiman Alshaya, Fahmy Gad Elsaid, Amr Yasser Mahmoud, Eman M Radwan, Ahmed RE Mahdy, Mohamed Ahmed Elian Sophy- Drug Discovery
- Pharmacology
- Molecular Medicine
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.