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The evaluation of RNAse active site model systems based on rigid steroid templates is described. Our preliminary work on steroid derived RNAse model systems showed that preorientation of guanidinum groups and one imidazole moiety leads to active compounds. We found that within the corticosterone derived steroid series, the C11-a-configurated compounds were superior to their b-diastereomers. In order to evaluate the influence of the conformational flexibility of the imidazole group, a flexible side chain was introduced at C17. The Fact that this more flexible imidazole group leads to a decrease in the hydrolytic behavior of the steroid derivative further validates our approach of establishing a preorientated RNAse model system for an efficient RNA hydrolysis.
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Tom
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89--99
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Bibliografia
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bwmeta1.element.baztech-article-BUJ2-0001-0010