Structure Function Relationships of Estrogenic Triphenylethylenes Related to Endoxifen and 4-Hydroxytamoxifen
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1,1,2-Triphenylethylene (TPE) derivatives were synthesized and evaluated against 17beta-estradiol (E2) for their estrogenic activity in MCF-7 human breast cancer cells and confirmed E2 as a class I estrogen and the TPEs as class II estrogens.Abstract:
Estrogens can potentially be classified into planar (class I) or nonplanar (class II) categories, which might have biological consequences 1,1,2-Triphenylethylene (TPE) derivatives were synthesized and evaluated against 17β-estradiol (E2) for their estrogenic activity in MCF-7 human breast cancer cells All TPEs were estrogenic and, unlike 4-hydroxytamoxifen (4OHTAM) and Endoxifen, induced cell growth to a level comparable to that of E2 All the TPEs increased ERE activity in MCF-7:WS8 cells with the order of potency as followed: E2 > 1,1-bis(4,4′-hydroxyphenyl)-2-phenylbut-1-ene (15) > 1,1,2-tris(4-hydroxyphenyl)but-1-ene (3) > Z 4-(1-(4-hydroxyphenyl)-1-phenylbut-1-en-2-yl)phenol (7) > E 4-(1-(4-hydroxyphenyl)-1-phenylbut-1-en-2-yl)phenol (6) > Z(4-(1-(4-ethoxyphenyl)-1-(4-hydroxyphenyl)but-1-en-2-yl)phenol (12) > 4-OHTAM Transient transfection of the ER-negative breast cancer cell line T47D:C4:2 with wild-type ER or D351G ER mutant revealed that all of the TPEs increased ERE activity in the cells expread more
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TL;DR: The 10-year and 15-year effects of various systemic adjuvant therapies on breast cancer recurrence and survival are reported and it is found that the cumulative reduction in mortality is more than twice as big at 15 years as at 5 years after diagnosis.
Journal ArticleDOI
Tamoxifen for Prevention of Breast Cancer: Report of the National Surgical Adjuvant Breast and Bowel Project P-1 Study
TL;DR: Tamoxifen decreases the incidence of invasive and noninvasive breast cancer and its use as a breast cancer preventive agent is appropriate in many women at increased risk for the disease.
Journal ArticleDOI
Tamoxifen for early breast cancer: An overview of the randomised trials
TL;DR: The absolute improvement in recurrence was greater during the first 5 years, whereas the improvement in survival grew steadily larger throughout the first 10 years, and these benefits appeared to be largely irrespective of age, menopausal status, daily tamoxifen dose, and of whether chemotherapy had been given to both groups.
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Tamoxifen for early breast cancer: an overview of the randomised trials. Early Breast Cancer Trialists' Collaborative Group
TL;DR: There have been many randomised trials of adjuvant tamoxifen among women with early breast cancer, and an updated overview of their results is presented in this paper, which approximately doubles the amount of evidence from trials of about 5 years of tamoxifier and, taking all trials together, on events occurring more than 5 years after randomisation.