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Influence of estradiol analogue on cell growth, morphology and death in esophageal carcinoma cells.
Biocell
December 2010
Department of Physiology, University of Pretoria, Pretoria, South Africa.
2-Methoxyestradiol-bis-sulphamate is a bis-sulphamoylated derivative of the naturally occurring 17-beta-estradiol metabolite namely 2-methoxyestradiol. 2-Methoxyestradiol-bis-sulphamate is regarded as a potential anticancer drug with increased antiproliferative activity when compared to 2-methoxyestradiol. The aim of this pilot in vitro study was to determine the influence of 2-methoxyestradiol-bis-sulphamate on cell growth, morphology and possible induction of certain types of cell death in the SNO esophageal carcinoma cell line.
View Article and Find Full Text PDFBreast cancer: are estrogen metabolites carcinogenic?
Climacteric
October 2007
University Women's Hospital of Tuebingen, Germany.
Certain estrogen metabolites can act as carcinogens in in vitro and animal experiments. The clinical relevance remains unclear. However, in the presence of factors that could influence estradiol metabolism, such as smoking or genetic polymorphisms, it seems prudent to prefer transdermal therapy to minimize the production of possible toxic metabolites.
View Article and Find Full Text PDFThe oestrogen metabolite 2-methoxyoestradiol alone or in combination with tumour necrosis factor-related apoptosis-inducing ligand mediates apoptosis in cancerous but not healthy cells of the human endometrium.
Endocr Relat Cancer
June 2007
Department of Obstetrics and Gynaecology, Faculty of Medicine, Pontificia Universidad Católica de Chile, Alameda 340, Santiago, Casilla 114-D, Chile.
Cancers of the reproductive tract account for 12% of all malignancies in women. As previous studies have shown that oestrogen metabolites can cause apoptosis, we characterised the effect of oestrogen and oestrogen metabolites on non-cancerous and cancerous human endometrial cells. Herein, we demonstrate that 2-methoxyoestradiol (2ME), but not 17beta-oestradiol, induces apoptosis in cancer cell lines and primary cultured tumours of endometrial origin.
View Article and Find Full Text PDFEffects of estrogens and metabolites on endometrial carcinogenesis in young adult mice initiated with N-ethyl-N'-nitro-N-nitrosoguanidine.
Cancer Lett
July 2004
Department of Pathology, Sasaki Institute, Sasaki Foundation, 2-2 Kanda-Surugadai, Chiyoda, Tokyo 101-0062, Japan.
The present study assessed effects of estrogens and their steroid metabolites on the endometrial carcinogenesis in young adult mice initiated with N-ethyl-N'-nitro-N-nitrosoguanidine (ENNG). A total of 272 female CD-1 (ICR) mice were used and equally divided into 17 groups. Mice were implanted cholesterol pellets to the back subcutis at 9 weeks of age.
View Article and Find Full Text PDFPharmacokinetics and efficacy of 2-methoxyoestradiol and 2-methoxyoestradiol-bis-sulphamate in vivo in rodents.
Br J Cancer
February 2004
1Endocrinology and Metabolic Medicine and Sterix Ltd, Faculty of Medicine, Imperial College, St Mary's Hospital, London W2 1NY, UK.
2-Methoxyoestradiol (2-MeOE2) is an endogenous oestrogen metabolite that inhibits the proliferation of cancer cells in vitro, and it is also antiangiogenic. In vivo 2-MeOE2, when administered at relatively high doses, inhibits the growth of tumours derived from breast cancer cells, sarcomas and melanomas. Sulphamoylated derivatives of 2-MeOE2 are more potent inhibitors of in vitro breast cancer cell growth than 2-MeOE2.
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