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Hydrophobicity of several rhodium(II) carboxylates correlated with their biologic activity.

作者信息

Howard R A, Sherwood E, Erck A, Kimball A P, Bear J L

出版信息

J Med Chem. 1977 Jul;20(7):943-6. doi: 10.1021/jm00217a016.

Abstract

Rhodium(II) carboxylates differ greatly in antitumor activity and toxicity depending on the properties of the carboxylate group (methoxyacetate, propionate, butyrate, etc.) involved. The solubility characteristics of rhodium(II) carboxylates correlate well with both the antitumor activity and toxicity that these compounds display. The amount of rhodium which is adsorbed by tumor cells in vitro also correlates with the partition coefficient of the rhodium(II) compounds studied. Survival and toxicity studies show rhodium(II) pentanoate to possess the highest therapeutic index against the Ehrlich ascites tumor strain and also show that lengthening the carboxylate R chain beyond the pentanoate reduces the drugs' therapeutic efficacy.

摘要

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