RESUMO
Various resistance mechanisms such as complex formation with DNA, tRNA and MDR1 p-glycoprotein were modified in bacteria and cancer cells in presence of pregnane, pyridoquinoline, and aza-oxafluorene derivatives. Interaction between the compounds, plasmid DNA and tRNA was shown and compared to the interaction with calf thymus DNA. Complex formation with MDR1 p-glycoprotein and drug accumulation increased in cancer cells. Both plasmid DNA and p-gp complex formation were related to the chemical structures of the resistance modifiers.
Assuntos
DNA/metabolismo , Fluorenos/química , Pregnanos/química , Quinolinas/química , RNA de Transferência/metabolismo , Membro 1 da Subfamília B de Cassetes de Ligação de ATP/metabolismo , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Relação Dose-Resposta a Droga , Interações Medicamentosas , Resistencia a Medicamentos Antineoplásicos , Fluorenos/farmacologia , Genes MDR , Humanos , Estrutura Molecular , Plasmídeos/genética , Plasmídeos/metabolismo , Pregnanos/farmacologia , Quinolinas/farmacologiaRESUMO
Anti MDR activity of a series of acridine, pyridoquinoline, quinoline and pyridine analogous amines was evaluated. Interesting activity is displayed by tricyclic compounds. Besides ring size, influence of the side chain was studied.