Synthesis and antiproliferative activity of epoxy and bromo compounds derived from estrone

Based on biological properties of epoxyquinols from natural sources, bromo and epoxyquinols derived from estrone were synthesized and screened against Fem-X, HeLa and K 562 cell lines. Evidence was found that the bromine atom and the epoxy moiety significantly increase the antiproliferative activity...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2001-08, Vol.11 (16), p.2197-2200
Hauptverfasser:	Milić, Dragana R., Kop, Tatjana, Juranić, Zorica, Gašić, Miroslav J., Šolaja, Bogdan A.
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic agents Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Biological and medical sciences Bromine - chemistry Cell Survival - drug effects Drug Screening Assays, Antitumor Epoxy Compounds - chemistry Estrone - chemical synthesis Estrone - chemistry Estrone - pharmacology General aspects HeLa Cells Humans K562 Cells Medical sciences Pharmacology. Drug treatments Tumor Cells, Cultured
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Beschreibung
Zusammenfassung:	Based on biological properties of epoxyquinols from natural sources, bromo and epoxyquinols derived from estrone were synthesized and screened against Fem-X, HeLa and K 562 cell lines. Evidence was found that the bromine atom and the epoxy moiety significantly increase the antiproliferative activity within the series. The synthesis and antiproliferative activity of some estrone-derived epoxy and bromo compounds are presented.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(01)00402-4