Design, synthesis and biological evaluation of estradiol-PEG-linked platinum(II) hybrid molecules: Comparative molecular modeling study of three distinct families of hybrids

[Display omitted] ▶ The synthesis of 17β-estradiol-PEG-linked platinum(II) hybrid molecules is reported. ▶ They are prepared from estrone in only 5 chemical steps with an overall yield of 22%. ▶ Molecular modeling study reveals distinct interactions with the estrogen receptor α. ▶ Lipophilicity and...

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Veröffentlicht in:	Steroids 2011, Vol.76 (1), p.94-103
Hauptverfasser:	Provencher-Mandeville, Josée, Debnath, Chhanda, Mandal, Sanat K., Leblanc, Valérie, Parent, Sophie, Asselin, Éric, Bérubé, Gervais
Format:	Artikel
Sprache:	eng
Schlagworte:	17 β-Estradiol-platinum(II) complex Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Binding Sites - drug effects Biological activity Biological and medical sciences Breast cancer Cell Line, Tumor Cell Proliferation - drug effects Cisplatin Dose-Response Relationship, Drug Drug Screening Assays, Antitumor Estradiol - chemistry Estrogen receptor Estrogen Receptor alpha - chemistry Fundamental and applied biological sciences. Psychology Gynecology. Andrology. Obstetrics Humans Mammary gland diseases Medical sciences Models, Molecular Molecular Conformation Molecular modeling Organometallic Compounds - chemical synthesis Organometallic Compounds - chemistry Organometallic Compounds - pharmacology Platinum - chemistry Polyethylene Glycols - chemistry Stereoisomerism Tumors Vertebrates: endocrinology
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