Salinosporamides and methods for use thereof

Details Salinosporamides and methods for use thereof Salinosporamides and methods for use thereof

C - Chemistry, Metallurgy

07

D

C07D 491/044 (2006.01) A61K 31/407 (2006.01)

Patent

CA 2530215

The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.

Selon la présente invention, certains produits de fermentation des souches d'actinomycète marin CNB392 et CNB476 constituent des inhibiteurs efficaces de cellules mammaliennes hyperproliférantes. Les souches CNB392 et CNB476 font partie de la famille micromonosporaceae, et l'épithète générique Salinospora a été proposé pour ce groupe marin obligatoire. Les produits de réaction élaborés au moyen de cette souche sont classifiés en tant que salinosporamides et ils présentent, spécifiquement, des avantages dans le traitement de troubles néoplasiques en raison de leur faible poids moléculaire, de leurs valeurs CI¿50? faibles, de leur puissance pharmaceutique élevée, et de leur sélectivité vis-à-vis des cellules cancéreuses par rapport aux champignons.

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