Erber, Sebastian and Angerer, Erwin von (1990) 2-phenylindole-linked nitroimidazoles as potential radiosensitizers for estrogen receptor positive tumors. Archiv der Pharmazie 323 (9), pp. 591-594.
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5-Hydroxy-2-(4-hydroxyphenyl)-3-methylindole was linked to nitroimidazoles by tetramethylene and hexamethylene spacer groups. Derivatives with a C₆-spacer (4c and 4d) exhibited high binding affinities for the estrogen receptor (RBA = 3.5; estradiol: 100), a prerequisite for a selective uptake by estrogen receptor positive tumors. Both compounds inhibited the growth of hormone-sensitive human MCF-7 mammary tumor cells at concentrations greater than 5 x 10⁻⁶ M, presumably due to the weak antiestrogenic effect observed in the mouse uterine weight test.
|Institutions:||Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)|
|Subjects:||500 Science > 570 Life sciences|
500 Science > 540 Chemistry & allied sciences
600 Technology > 610 Medical sciences Medicine
|Refereed:||Yes, this version has been refereed|
|Created at the University of Regensburg:||Yes|
|Owner:||Prof. Armin Buschauer|
|Deposited On:||03 Nov 2008 15:34|
|Last Modified:||05 Aug 2009 13:48|