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| Visagie,Michelle Helen; Jaiswal,Seema Rummurat; Joubert,Anna Margaretha. |
| BACKGROUND: Computer-based technology is becoming increasingly essential in biological research where drug discovery programs start with the identification of suitable drug targets. 2-Methoxyestradiol (2ME2) is a 17ß-estradiol metabolite that induces apoptosis in various cancer cell lines including cervical cancer, breast cancer and multiple myeloma. Owing to 2ME2's poor in vivo bioavailability, our laboratory in silico-designed and subsequently synthesized a novel 2ME2 analogue, 2-ethyl-3-O-sulphamoyl-estra-1,3,5(10),15-tetraen-17-ol (ESE-15-ol), using receptor- and ligand molecular modeling. In this study, the biological effects of ESE-15-ol (180 nM) and its parent molecule, 2ME2 (1 μM), were assessed on morphology and apoptosis induction in... |
| Tipo: Journal article |
Palavras-chave: Morphology; Apoptosis; Cervical cancer; ESE-15-ol. |
| Ano: 2016 |
URL: http://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0716-97602016000100043 |
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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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