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| Item type: | Article | ||||
|---|---|---|---|---|---|
| Journal or Publication Title: | Journal of Medicinal Chemistry | ||||
| Publisher: | American Chemical Society | ||||
| Volume: | 38 | ||||
| Number of Issue or Book Chapter: | 12 | ||||
| Page Range: | pp. 2070-2079 | ||||
| Date: | 1995 | ||||
| Additional Information (public): | 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) | ||||
| Institutions: | Chemistry and Pharmacy > Institute of Pharmacy > Alumni or Retired Professors > Prof. Schönenberger | ||||
| Projects (Historical): | SFB 234 | ||||
| Identification Number: |
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| 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 Decimal Classification: | 500 Science > 540 Chemistry & allied sciences | ||||
| Status: | Published | ||||
| Refereed: | Yes, this version has been refereed | ||||
| Created at the University of Regensburg: | Yes | ||||
| Item ID: | 17707 |
Abstract
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 ...
Abstract
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.
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