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| Item type: | Article | ||||
|---|---|---|---|---|---|
| Journal or Publication Title: | European journal of medicinal chemistry | ||||
| Publisher: | Elsevier | ||||
| Volume: | 17 | ||||
| Number of Issue or Book Chapter: | 6 | ||||
| Page Range: | pp. 491-495 | ||||
| Date: | 1982 | ||||
| Additional Information (public): | CAN 98:119150 1-3 Pharmacology 84609-02-9; 84609-03-0 Role: PROC (Process) (estrogen receptor binding of); 57660-12-5P; 84608-99-1P Role: RCT (Reactant), SPN (Synthetic preparation), PREP (Preparation), RACT (Reactant or reagent) (prepn. and acetoxylation and methoxylation of); 57660-16-9P; 84609-00-7P Role: RCT (Reactant), SPN (Synthetic preparation), PREP (Preparation), RACT (Reactant or reagent) (prepn. and acetylation of); 588-59-0DP Role: SPN (Synthetic preparation), PREP (Preparation) (prepn. and antitumor activity and estrogen receptor binding of); 84608-97-9P; 84609-01-8P Role: BAC (Biological activity or effector, except adverse), BSU (Biological study, unclassified), SPN (Synthetic preparation), THU (Therapeutic use), BIOL (Biological study), PREP (Preparation), USES (Uses) (prepn. and antitumor activity of); 5965-06-0P; 57660-13-6P; 70424-18-9P; 84608-98-0P Role: SPN (Synthetic preparation), PREP (Preparation) (prepn. and estrogen receptor binding of); 130-79-0; 76473-06-8 Role: RCT (Reactant), RACT (Reactant or reagent) (reaction of, with benzylammonium chloride); 3287-99-8 Role: RCT (Reactant), RACT (Reactant or reagent) (reaction of, with dimethoxydiethylstilbenes); 26264-09-5 Role: BIOL (Biological study) (reaction with diethylvinylene-bis(phenyl)diacetate) | ||||
| Institutions: | Chemistry and Pharmacy > Institute of Pharmacy > Alumni or Retired Professors > Prof. Schönenberger | ||||
| Projects (Historical): | SFB 234 | ||||
| Identification Number: |
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| Keywords: | Uterus (estrogen receptors of, stilbene derivs. binding by, antitumor activity in relation to) Receptors Role: BIOL (Biological study) (for estrogens, of uterus, stilbene derivs. binding by, antitumor activity in relation to) Estrogens Role: BIOL (Biological study) (receptors for, of uterus, stilbene derivs. binding by, antitumor activity in relation to) Neoplasm inhibitors (carcinoma, mammary, stilbene derivs. as, in human) Cytoplasm (cytosol, estrogen receptors of, of uterus, stilbene derivs. binding by, antitumor activity in relation to) Molecular structure-biological activity relationship (estrogen receptor-binding, of stilbene derivs.) Mammary gland (neoplasm, carcinoma, (diethylcyclopropanediyl)bis(phenyl) diacetates for treatment of human) ethylcyclopropanediylbisphenyl diacetate antitumor stilbene analog mammary carcinoma estrogen receptor stilbene analog | ||||
| 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: | 17634 |
Abstract
trans-[3,3'-] [84609-01-8] And trans-[4,4'-(1,2-diethyl-1,2-cyclopropanediyl)-bis-(phenyl)] diacetate (I) [84608-97-9] and their 3,3-dichloro derivs. were prepd., and their effect on postmenopausal, hormone-dependent human mammary carcinoma and estrogen receptor affinities in calf uterus cytosol were detd. Meta-substituted compds. exhibited a lower receptor affinity than their para-substituted ...
Abstract
trans-[3,3'-] [84609-01-8] And trans-[4,4'-(1,2-diethyl-1,2-cyclopropanediyl)-bis-(phenyl)] diacetate (I) [84608-97-9] and their 3,3-dichloro derivs. were prepd., and their effect on postmenopausal, hormone-dependent human mammary carcinoma and estrogen receptor affinities in calf uterus cytosol were detd. Meta-substituted compds. exhibited a lower receptor affinity than their para-substituted counterparts. Introduction of a cyclopropyl moiety into the stilbenes increased estrogen receptor affinity but to a lesser extent than did introduction of an epoxide group. Comparison of cyclopropyl and 3,3-dichlorocyclopropyl analogs revealed a greater receptor affinity in the cyclopropanes. The 2 cyclopropyl analogs exhibited marked antitumor activity on human mammary carcinomas transplanted in nude mice. The effect of these compds. was at least comparable to that of tamoxifen.
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