PMID: 6813499Sep 1, 1982Paper

1,1,2-triphenylbut-1-enes: relationship between structure, estradiol receptor affinity, and mammary tumor inhibiting properties

Journal of Medicinal Chemistry
M R SchneiderH P Fortmeyer


1,1,2-Triphenylbut-1-enes, which are substituted with acetoxy groups on one, two, or three aromatic rings in the para and/or meta positions, were synthesized. The identity of the occurring E and Z isomers were established by 1H NMR spectroscopy. A study on structure-activity relationships was carried out with regard to estradiol receptor affinity and to inhibiting effects on the growth of a postmenopausal human mammary carcinoma implanted in nude mice. The para-substituted compounds generally exhibited a higher receptor affinity and a better antitumor activity than the corresponding meta-substituted ones. The E isomers were superior to the respective Z isomers in those two properties. The tumor-inhibiting effect of the mono- and disubstituted compounds was better than that of the trisubstituted ones. Except for the trisubstituted compounds, they all show a good correlation between estradiol receptor affinity and antitumor activity. One of the compounds was also tested on the 9,10-dimethylbenz[a]-anthracene-induced, hormone-dependent mammary carcinoma of the Sprague-Dawley rat, and the results corresponded to those obtained in the xenograft tumor.


Aug 26, 1998·International Journal of Cancer. Journal International Du Cancer·Y LavieM C Cabot
Jan 1, 1986·Journal of Cancer Research and Clinical Oncology·M R SchneiderW Amselgruber
Jan 1, 1986·Journal of Cancer Research and Clinical Oncology·M R Schneider
Mar 1, 1993·Biulleten' eksperimental'noĭ biologii i meditsiny·E N Kareva, O I Kostyleva
Feb 1, 1995·Biulleten' eksperimental'noĭ biologii i meditsiny·N V SergeevN Iu Tkacheva
Jun 1, 1988·Journal of Steroid Biochemistry·E R DeSombreA Hughes
Mar 1, 1992·The Journal of Steroid Biochemistry and Molecular Biology·E von Angerer, S Erber
Jan 1, 1986·Journal of Cancer Research and Clinical Oncology·M R SchneiderW P Brade
Nov 26, 2015·Memórias do Instituto Oswaldo Cruz·Nicolli Bellotti de SouzaAntoniana Ursine Krettli
Mar 10, 2007·Bioorganic & Medicinal Chemistry Letters·Isamu ShiinaYoshimune Hasome
Aug 27, 2014·ChemMedChem·Alane Cabral de OliveiraLetícia V Costa-Lotufo
May 1, 1987·Archiv der Pharmazie·J Strohmeier, E von Angerer
Nov 10, 2007·Dalton Transactions : an International Journal of Inorganic Chemistry·Elizabeth Anne HillardGérard Jaouen
Apr 28, 2006·Bioorganicheskaia khimiia·L E GolubovskaiaV M Rzheznikov

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