Vários estudos têm mostrado o potencial citotóxico de derivados da nor-β-lapachona contra células tumorais. Considerando a nor-β-lapachona um importante protótipo, uma série inédita de nor-β-lapachonas substituídas em C-3 foi sintetizada através de uma nova metodologia sintética envolvendo intermediário sintético 3-hidróxi-nor-β-lapachona para o acoplamento de alguns nucleófilos contendo núcleos derivados de carboidratos ou 2H-pirazóis. Todos os derivados foram avaliados frente a quatro linhagens de células tumorais. Duas das substâncias apresentaram moderada citotoxicidade, enquanto as demais inibiram fortemente todas as linhagens tumorais testadas.Several studies have demonstrated the cytotoxic potential of nor-β-lapachone derivative against cancer cells. Considering nor-β-lapachone as an important prototype, a set of new 3-substituted nor-β-lapachones was synthesized by a new synthetic route that involves the use of synthetic intermediate generated for coupling with several nucleophiles containing the carbohydrate and 2H-pyrazole substituent moieties. All the compounds were screened against four tumor cell lines. Two of the compounds showed moderate cytotoxicity, while the other compounds strongly inhibit all tested cancer cell lines.
Synthesis of Fused Chromene-1,4-naphthoquinones via Ring-Closing Metathesis and Knoevenagel-Electrocyclization under Acid Catalysis and Microwave Irradiation. -Two strategies for the synthesis of fused chromene-1,4-naphthoquinones are described. The first route is based on the Knoevenagel condensation/cyclization of 2-hydroxynaphthoquinones (I) with ,-unsaturated carbonyl compounds. The second strategy is based on Grubbs ring closing metathesis as key step. -(DA ROCHA, D. R.; MOTA, K.; DA SILVA, I. M. C. B.; FERREIRA, V. F.; FERREIRA, S. B.; DA SILVA*, F. D. C.; Tetrahedron 70 (2014) 20, 3266-3270, http://dx.
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