RESUMO
An efficient method is proposed for obtaining tetrahydrobenzo[a]xanthene-11-ones and tetrahydro-[1,3]-dioxolo[4,5-b]xanthen-9-ones. The method is based on the use of p-sulfonic acid calix[n]arenes as catalysts under solvent-free conditions. The antiproliferative activity of fifty-nine xanthenones against six human cancer cells was studied. The capacity of all compounds to inhibit cancer cell growth was dependent on the histological origin of the cells. QSAR studies indicate that among compounds derived from ß-naphthol the most efficient compounds against glioma (U251) and renal (NCI-H460) cancer cells are those having higher hydrogen bonding donor ability.
Assuntos
Antineoplásicos/farmacologia , Calixarenos/química , Relação Quantitativa Estrutura-Atividade , Xantenos/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Catálise , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Células HT29 , Humanos , Células MCF-7 , Estrutura Molecular , Xantenos/síntese química , Xantenos/químicaAssuntos
Animais , Cães , Eutanásia Animal , Raiva , Vírus da Raiva , Avaliação da Pesquisa em Saúde , Saúde PúblicaAssuntos
Animais , Cães , Eutanásia Animal , Raiva , Vírus da Raiva , Avaliação da Pesquisa em Saúde , Saúde PúblicaRESUMO
A diastereoselective three-component cascade reaction, catalyzed by p-sulfonic acid calix[4]arene, provides a unique method to access diverse julolidine derivatives in high yields. Additionally, the reaction was also monitored by mass spectrometry and the mechanistic pathway uncovered.