Document Detail

Influence of cyclopropyl antiestrogens on the cell cycle kinetics of MCF-7 human breast cancer cells.
MedLine Citation:
PMID:  8669818     Owner:  NLM     Status:  MEDLINE    
Five cyclopropyl compounds, previously shown to exhibit pure antiestrogenic activity in the mouse uterotropic assay and antiproliferative activity of MCF-7 human breast cancer cells in culture, were examined for their influence on the cell cycle kinetics of MCF-7 cells. The DNA-histogram of a single cell suspension was obtained on Coulter Epics V after fixing the cells in 70 % ethyl alcohol and staining in propidium iodide. Tamoxifen increased the percentage of cells in G1-phase with a concomitant decrease in percentage of cells in S-phase, in an estradiol reversible manner. Cyclopropyl compound 7a increased the percentage of cells in G1-phase, in an estradiol-irreversible manner. Further, compounds 5a, 5c, 7a and 7b decreased the percentage of cells in S-phase and increased percentage of cells in the G2M-phase, in an estradiol-irreversible manner. Of the five cyclopropyl compounds tested, only 4d had no influence on the cytokinetic parameters, even though this compound was found to exhibit antiproliferative activity on MCF-7 cells equal to that of tamoxifen. In conclusion, all of the cyclopropyl compounds, except 4d, altered cell cycle parameters of MCF-7 cells in a manner different than that of tamoxifen. Thus, the results of this study indicate that, although these cyclopropyl compounds are antiestrogenic, they produce antiproliferative activity by a distinct mechanism of action in estrogen receptor positive breast cancer cells.
P T Jain; J T Pento; R A Magarian
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Publication Detail:
Type:  Comparative Study; Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  Anticancer research     Volume:  15     ISSN:  0250-7005     ISO Abbreviation:  Anticancer Res.     Publication Date:    1995 Nov-Dec
Date Detail:
Created Date:  1996-08-07     Completed Date:  1996-08-07     Revised Date:  2007-11-14    
Medline Journal Info:
Nlm Unique ID:  8102988     Medline TA:  Anticancer Res     Country:  GREECE    
Other Details:
Languages:  eng     Pagination:  2529-32     Citation Subset:  IM    
Department of Pharmacology and Toxicology, College of Pharmacy, University of Oklahoma Health Sciences Center, Oklahoma City 73190, USA.
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MeSH Terms
Adenocarcinoma / pathology*
Antineoplastic Agents, Hormonal / chemistry,  pharmacology*
Breast Neoplasms / pathology*
Cell Cycle / drug effects*
Cyclopropanes / chemistry,  pharmacology*
DNA, Neoplasm / analysis
Estradiol / pharmacology
Estrogen Antagonists / chemistry,  pharmacology*
Neoplasms, Hormone-Dependent / pathology*
Tamoxifen / pharmacology
Tumor Cells, Cultured
Grant Support
Reg. No./Substance:
0/Antineoplastic Agents, Hormonal; 0/Cyclopropanes; 0/DNA, Neoplasm; 0/Estrogen Antagonists; 0/Estrogens; 10540-29-1/Tamoxifen; 50-28-2/Estradiol

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