Effects of synthetic bis-beta-chloroethylamine estrogen derivatives on proliferation of skin sarcoma cells.

Abstract

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.

• Authors: A V Semeikin, V M Rzheznikov, E E Mayatskaya, Z S Smirnova
• Journal: Bulletin of experimental biology and medicine (Bull Exp Biol Med) Vol. 129 Issue 6 Pg. 592-4 (Jun 2000) ISSN: 0007-4888 [Print] United States
• PMID: 11022259 (Publication Type: Journal Article)

Chemical References

• Antineoplastic Agents, Hormonal
• Estradiol Congeners
• Ethylamines
• Nitrogen Mustard Compounds
• estradiol mustard

Topics

• Animals
• Antineoplastic Agents, Hormonal (chemistry, pharmacology)
• Cell Division (drug effects)
• Dose-Response Relationship, Drug
• Estradiol Congeners (chemistry, pharmacology)
• Ethylamines (pharmacology)
• Fibroblasts (drug effects)
• Mice
• Molecular Structure
• Nitrogen Mustard Compounds (pharmacology)
• Sarcoma
• Skin Neoplasms
• Tumor Cells, Cultured