| Autor: |
de Lucas Chazin, Eliza, de Souza Sanches, Paola, Brazil Lindgren, Eric, Vellasco Júnior, Walcimar Trindade, Pinto, Laine Celestino, Rodríguez Burbano, Rommel Mario, Yoneda, Julliane Diniz, Zaccur Leal, Kátia, Brandão Gomes, Claudia Regina, Wardell, James Lewis, Silva Veloso Wardell, Solange Maria, Carvalho Montenegro, Raquel, Alves Vasconcelos, Thatyana Rocha |
| Předmět: |
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| Zdroj: |
Molecules; Feb2015, Vol. 20 Issue 2, p1968-1983, 16p, 3 Diagrams, 2 Charts |
| Abstrakt: |
With the aim of discovering new anticancer agents, we have designed and synthesized novel 6-hydroxy-benzo[d][1,3]oxathiol-2-one Schiff bases. The synthesis started with the selective nitration at 5-position of 6-hydroxybenzo[d][1,3]oxathiol-2-one (1) leading to the nitro derivative 2. The nitro group of 2 was reduced to give the amino intermediate 3. Schiff bases 4a–r were obtained from coupling reactions between 3 and various benzaldehydes and heteroaromatic aldehydes. All the new compounds were fully identified and characterized by NMR (1H and 13C) and specifically for 4q by X-ray crystallography. The in vitro cytotoxicity of the compounds was evaluated against cancer cell lines (ACP-03, SKMEL-19 and HCT-116) by using MTT assay. Schiff bases 4b and 4o exhibited promising cytotoxicity against ACP-03 and SKMEL-19, respectively, with IC50 values lower than 5 μM. This class of compounds can be considered as a good starting point for the development of new lead molecules in the fight against cancer. [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
| Externí odkaz: |
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