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J Nat Prod ; 76(9): 1523-7, 2013 Sep 27.
Artigo em Inglês | MEDLINE | ID: mdl-24050204

RESUMO

Three new compounds named leporizines A-C have been isolated from an Aspergillus sp. strain. Their structures were elucidated by analysis of 1D and 2D NMR spectra. Leporizines A and B were isolated during dereplication of hits from a high-throughput screening campaign for correctors of the cystic fibrosis transmembrane conductance regulator (CFTR), and leporizine C was isolated while preparing additional material for characterization of leporizines A and B. CFTR activity observed for leporizines A and B was highly correlated with cell toxicity and was determined to be a nonspecific effect. Leporizine C was not cytotoxic to cells and did not elicit a response in the CFTR assays. To the best of our knowledge, leporizines A-C represent the first examples of this unusual epithiodiketopiperazine skeleton.


Assuntos
Antineoplásicos/isolamento & purificação , Aspergillus/química , Dicetopiperazinas/isolamento & purificação , Antineoplásicos/química , Antineoplásicos/farmacologia , Regulador de Condutância Transmembrana em Fibrose Cística/efeitos dos fármacos , Dicetopiperazinas/química , Dicetopiperazinas/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Células Hep G2 , Humanos , Estrutura Molecular , Montana , Mutação , Ressonância Magnética Nuclear Biomolecular , Mucosa Respiratória
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