Evaluation of novel synthesized thiazole derivatives as potential aromatase inhibitors against breast cancer

Abstract

<b>Background:</b> 4-Methylacetophenone is used in the preparation of starting materials, 4-methylphenacyle bromide (<b>2</b>) and 4-methylacetophenone thiosemicarbazole (<b>3</b>). <b>Results:</b> 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 <b>5-8</b> respectively. <b>Conclusion:</b> Compounds <b>5-8</b> were investigated for their cytotoxic activity on MCF-7 and normal breast cells. Active compounds were found and in contrast to staurosporine, compound <b>8</b> 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.