Effects of synthetic bis-beta-chloroethylamine estrogen derivatives on proliferation of skin sarcoma cells.
The effects of four new synthetic bis-beta-chloroethylamine-containing estrogens and known cytostatic agents chlorophenacyl and estradiol mustard were compared on monolayer cultures of transformed L-929 fibroblasts (from murine skin sarcoma). The drugs within the concentration range of 10(-5)-5 10(-7)M inhibited proliferation of cultured cells by 67%. Chlorophenacyl displayed the least antiproliferative activity (15% inhibition at 10(-5) M). Steroid nucleus introduced into the molecule enhanced antiproliferative activity of test drug in comparison with chlorophenacyl, probably due to accumulation of the hormone-cytostatic molecules in cells. Estradiol had no effect on proliferative activity of L-929 cells, and no specific estrogen-binding sites were found in cultured transformed fibroblasts. The antiproliferative effect of hormone-cytostatics on this culture is not mediated via specific interactions with estrogen receptors.
Semeikin
A V
AV
Department of Molecular Pharmacology and Radiobiology, Russian State Medical University, Moscow.
Rzheznikov
V M
VM
Mayatskaya
E E
EE
Smirnova
Z S
ZS
D000818:Animals; D018931:Antineoplastic Agents, Hormonal / Q000737:chemistry / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D045166:Estradiol Congeners / Q000737:chemistry / Q000494:pharmacology*; D005021:Ethylamines / Q000494:pharmacology*; D005347:Fibroblasts / Q000187:drug effects*; D051379:Mice; D015394:Molecular Structure; D009588:Nitrogen Mustard Compounds / Q000494:pharmacology; D012509:Sarcoma; D012878:Skin Neoplasms; D014407:Tumor Cells, Cultured
D018931:Antineoplastic Agents, Hormonal; D045166:Estradiol Congeners; D005021:Ethylamines; D009588:Nitrogen Mustard Compounds; C023758:estradiol mustard