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À propos de : Synthesis and Pharmacological Evaluation of 1H-Imidazoles as Ligands for theEstrogen Receptor and Cytotoxic Inhibitors of the Cyclooxygenase        

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  • Synthesis and Pharmacological Evaluation of 1H-Imidazoles as Ligands for theEstrogen Receptor and Cytotoxic Inhibitors of the Cyclooxygenase
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  • The 1H-imidazoles 7a−e were synthesized and tested for biological activity in vitro. The resultspointed to a clear structure−activity relationship. The introduction of an ethyl chain at C5 ofthe 1,2,4-tris(4-hydroxyphenyl)-1H-imidazole 7a caused hormonal activity in estrogen receptorpositive MCF-7-2a cells. An o-chlorine substituent in the phenolic rings at C2 and C4 as realizedin 7b and 7c increased the antiproliferative effects against human breast cancer cell linesMCF-7 and MDA-MB 231. Additionally, both compounds showed strong inhibitory effects oncyclooxygenase enzymes. Therefore, a mode of action including the interference in thearachidonic acid cascade might be possible.
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