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  • Title: Synthesis and pharmacological evaluation of 1H-imidazoles as ligands for the estrogen receptor and cytotoxic inhibitors of the cyclooxygenase.
    Author: Wiglenda T, Ott I, Kircher B, Schumacher P, Schuster D, Langer T, Gust R.
    Journal: J Med Chem; 2005 Oct 06; 48(20):6516-21. PubMed ID: 16190777.
    Abstract:
    The 1H-imidazoles 7a-e were synthesized and tested for biological activity in vitro. The results pointed to a clear structure-activity relationship. The introduction of an ethyl chain at C5 of the 1,2,4-tris(4-hydroxyphenyl)-1H-imidazole 7a caused hormonal activity in estrogen receptor positive MCF-7-2a cells. An o-chlorine substituent in the phenolic rings at C2 and C4 as realized in 7b and 7c increased the antiproliferative effects against human breast cancer cell lines MCF-7 and MDA-MB 231. Additionally, both compounds showed strong inhibitory effects on cyclooxygenase enzymes. Therefore, a mode of action including the interference in the arachidonic acid cascade might be possible.
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