Premium
2‐Phenylindole‐linked Nitroimidazoles as Potential Radiosensitizers for Estrogen Receptor Positive Tumors
Author(s) -
Erber Sebastian,
Angerer Erwin Von
Publication year - 1990
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.19903230907
Subject(s) - chemistry , estrogen receptor , estrogen , selective estrogen receptor modulator , pharmacology , medicine , cancer , breast cancer
S‐Hydroxy‐2‐(4‐hydroxyphenyl)‐3‐methylindole was linked to nitroimidazoles by tetramethylene and hexamethylene spacer groups. Derivatives with a C 6 ‐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 > 5×10 −6 M, presumably due to the weak antiestrogenic effect observed in die mouse uterine weight test.