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| Mqoco,Thandi; Marais,Sumari; Joubert,Annie. |
| 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. A dose-dependent study (0.2-1.0µM) was conducted with an exposure time of 24 hours. Data revealed that 2-methoxyestradiol-bis-sulphamate reduced cell numbers statistically significantly to 74% after exposure to 0.4µM of the drug.... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Cancer; Apoptosis; Autophagy. |
| Ano: 2010 |
URL: http://www.scielo.org.ar/scielo.php?script=sci_arttext&pid=S0327-95452010000300003 |
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| Repsold,Lisa; Mqoco,Thandi; Wolmarans,Elize; Nkandeu,Sandra; Theron,Joji; Piorkowski,Tomek; du Toit,Peet; van Papendorp,Dirk; Joubert,Annie Margaretha. |
| BACKGROUND: Novel, in silico-designed anticancer compounds were synthesized in our laboratory namely, 2-ethyl-3-O-sulphamoyl-estra-1,3,5(10),15-tetraen-17-ol (ESE-15-ol) and 2-ethyl-3-O-sulphamoyl-estra-1,3,5(10)16-tetraene (ESE-16). These compounds were designed to have improved bioavailability when compared to their source compound, 2-methoxyestradiol. This theoretically would be due to their increased binding affinity to carbonic anhydrase II, present in erythrocytes. Since the novel compounds under investigation are proposed to be transported within erythrocytes bound to carbonic anhydrase II, the morphological effect which they may exert on whole blood and erythrocytes is of great significance. A secondary outcome included revision of previously... |
| Tipo: Journal article |
Palavras-chave: Whole blood; Morphology; ESE-15-ol; ESE-16; Anticancer; Erythrocytes. |
| Ano: 2014 |
URL: http://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0716-97602014000100039 |
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