Dokumentenart: | Artikel | ||||
---|---|---|---|---|---|
Titel eines Journals oder einer Zeitschrift: | Journal of Medicinal Chemistry | ||||
Verlag: | American Chemical Society | ||||
Band: | 38 | ||||
Nummer des Zeitschriftenheftes oder des Kapitels: | 12 | ||||
Seitenbereich: | S. 2070-2079 | ||||
Datum: | 1995 | ||||
Zusätzliche Informationen (Öffentlich): | CAN 123:46660 78-7 Inorganic Chemicals and Reactions 10025-99-7 (Potassium tetrachloroplatinate(2-); 83363-98-8; 164411-34-1 Role: RCT (Reactant), RACT (Reactant or reagent) (for prepn. of platinum(II) chloro bis(dichlorohydroxyphenyl)ethylenediamine complex); 164411-32-9P; 164411-33-0P Role: RCT (Reactant), SPN (Synthetic preparation), PREP (Preparation), RACT (Reactant or reagent) (for prepn. of platinum(II) chloro bis(dichlorohydroxyphenyl)ethylenediamine complex); 105856-23-3; 105928-14-1; 111086-58-9; 111112-21-1 Role: BAC (Biological activity or effector, except adverse), BSU (Biological study, unclassified), BIOL (Biological study) (prepn., estradiol receptor affinity, and estrogenic activity of diastereomeric platinum(II) chloro bis(dichlorohydroxyphenyl)ethylenediamine complexes); 82772-86-9P; 82772-87-0P; 82772-89-2P; 82772-90-5P; 164411-30-7P; 164411-31-8P Role: BAC (Biological activity or effector, except adverse), BSU (Biological study, unclassified), RCT (Reactant), SPN (Synthetic preparation), BIOL (Biological study), PREP (Preparation), RACT (Reactant or reagent) (prepn., estradiol receptor affinity, and estrogenic activity of diastereomeric platinum(II) chloro bis(dichlorohydroxyphenyl)ethylenediamine complexes); 164411-28-3P; 164411-29-4P; 164577-11-1P; 164577-12-2P; 164577-13-3P; 164577-14-4P Role: BAC (Biological activity or effector, except adverse), BSU (Biological study, unclassified), SPN (Synthetic preparation), BIOL (Biological study), PREP (Preparation) (prepn., estradiol receptor affinity, and estrogenic activity of diastereomeric platinum(II) chloro bis(dichlorohydroxyphenyl)ethylenediamine complexes) | ||||
Institutionen: | Chemie und Pharmazie > Institut für Pharmazie > Entpflichtete oder im Ruhestand befindliche Professoren > Prof. Schönenberger | ||||
Projekte: | SFB 234 | ||||
Identifikationsnummer: |
| ||||
Stichwörter / Keywords: | Configuration Conformation and Conformers (prepn., estradiol receptor affinity, and estrogenic activity of diastereomeric platinum(II) chloro bis(dichlorohydroxyphenyl)ethylenediamine complexes) Estrogens Role: BAC (Biological activity or effector, except adverse), BSU (Biological study, unclassified), BIOL (Biological study) (prepn., estradiol receptor affinity, and estrogenic activity of diastereomeric platinum(II) chloro bis(dichlorohydroxyp Estrogen receptors Role: BSU (Biological study, unclassified), BIOL (Biological study) (prepn., estradiol receptor affinity, and estrogenic activity of diastereomeric platinum(II) chloro bis(dichlorohydroxyphenyl)ethylenediamine complexes) Receptors Role: BSU (Biological study, unclassified), BIOL (Biological study) (estrogen, prepn., estradiol receptor affinity, and estrogenic activity of diastereomeric platinum(II) chloro bis(dichlorohydroxyphenyl)ethylenediamine complexes) Molecular structure-biological activity relationship (estrogen receptor-binding, prepn., estradiol receptor affinity, and estrogenic activity of diastereomeric platinum(II) chloro bis(dichlorohydroxyphenyl)ethylenediamine complexes) platinum chloro hydroxyphenylethylenediamine estrogen receptor binding ethylenediamine deriv platinum complex estrogen activity | ||||
Dewey-Dezimal-Klassifikation: | 500 Naturwissenschaften und Mathematik > 540 Chemie | ||||
Status: | Veröffentlicht | ||||
Begutachtet: | Ja, diese Version wurde begutachtet | ||||
An der Universität Regensburg entstanden: | Ja | ||||
Dokumenten-ID: | 17707 |
Zusammenfassung
N-Monoalkylated (Et) and N,N'-dialkylated (Me and Et) 1,2-bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamines and their dichloroplatinum(II) complexes were synthesized, and their configuration and conformational behavior were 1H-NMR spectroscopically clarified. The latter was brought in relation to their relative binding affinity (RBA) to the estrogen receptor as well as to their estrogenic ...
Zusammenfassung
N-Monoalkylated (Et) and N,N'-dialkylated (Me and Et) 1,2-bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamines and their dichloroplatinum(II) complexes were synthesized, and their configuration and conformational behavior were 1H-NMR spectroscopically clarified. The latter was brought in relation to their relative binding affinity (RBA) to the estrogen receptor as well as to their estrogenic potency. In contrast to the RR/SS-configurated diamines, the R/S-configurated ones showed marked estrogenic properties which correlate with the RBA's. In the related R/S-configurated complexes the estrogenic activity is detd. by the same structural requirements as in the diamine series. However, a correlation between RBA's and estrogenic potencies is missing. The connection between spatial structure and activity is discussed using a drug-receptor model recently proposed by Holtje and Dall.
Metadaten zuletzt geändert: 24 Mai 2018 12:18