Studies for Structure-Activities Relationships of Reveromycin A : An Inhibitor of Eukaryotic Cell Growth

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Reveromycin A is a novel polyketide-type antibiotic produced by Streptomyces sp. and inhibits mitogenic activity induced by the epidermal growth factor in a mouse epidermal keratinocyte. The characteristic structural features of reveromycin A include a 1,7-dioxaspiro[5.5]undecane moiety, that is, the 6,6-spiroacetal system bearing a hemisuccinate, two alkenyl carboxylic acids, and methyl and n-butyl groups. Various derivatives of reveromycin A were prepared and their inhibitory effects on both isoleucyl-tRNA synthetase activity and in vitro protein synthesis, and activities on the morphological reversion of src^<ts> NRK cells were assayed. It was clarified that the C5 hydroxyl group and C24 carboxyl group were particularly important for these activities.