synthesis, dna binding and topoisomerase i inhibition activity of thiazacridine and imidazacridine derivatives
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ID: 216132
2013
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Abstract
Thiazacridine and imidazacridine derivatives have shown promising results as tumors suppressors in some cancer cell lines. For a better understanding of the mechanism of action of these compounds, binding studies of 5-acridin-9-ylmethylidene-3-amino-2-thioxo-thiazolidin-4-one, 5-acridin-9-ylmethylidene-2-thioxo-thiazolidin-4-one, 5-acridin-9-ylmethylidene-2-thioxo-imidazolidin-4-one and 3-acridin-9-ylmethyl-thiazolidin-2,4-dione with calf thymus DNA (ctDNA) by electronic absorption and fluorescence spectroscopy and circular dichroism spectroscopy were performed. The binding constants ranged from 1.46 × 104 to 6.01 × 104 M−1. UV-Vis, fluorescence and circular dichroism measurements indicated that the compounds interact effectively with ctDNA, both by intercalation or external binding. They demonstrated inhibitory activities to human topoisomerase I, except for 5-acridin-9-ylmethylidene-2-thioxo-1,3-thiazolidin-4-one. These results provide insight into the DNA binding mechanism of imidazacridines and thiazacridines.
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lafayette2013moleculessynthesis,
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| Authors | ;Elizabeth Almeida Lafayette;Sinara Mônica Vitalino de Almeida;Marina Galdino da Rocha Pitta;Eduardo Isidoro Carneiro Beltrão;Teresinha Gonçalves da Silva;Ricardo Olímpio de Moura;Ivan da Rocha Pitta;Luiz Bezerra de Carvalho;Maria do Carmo Alves de Lima |
| Journal | Journal of ethnopharmacology |
| Year | 2013 |
| DOI |
10.3390/molecules181215035
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| URL | |
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