Berberine and several structurally-related analogs were evaluated as inhibitors of topoisomerase I andll. The pharmacological activity of protoberberines exhibited a strong dependence upon the type and location of substituents. Several of these alkaloids exhibited activity as inhibitors of topoisomerase ll. Among the bicyclic heterocyclic analogs evaluated, none exhibited similar potency to berberirubine as an inhibitor of topoisomerase ll. Of tbe analogs studied, 2,3-desmethylene-9,10- desmethylberberine was the most potent inhibitor of topoisomerase I when assayed in vitro.
Protoberberine alkaloids and related compounds as dual inhibitors of mammalian topoisomerase I and II
GATTO, BARBARA;
1994
Abstract
Berberine and several structurally-related analogs were evaluated as inhibitors of topoisomerase I andll. The pharmacological activity of protoberberines exhibited a strong dependence upon the type and location of substituents. Several of these alkaloids exhibited activity as inhibitors of topoisomerase ll. Among the bicyclic heterocyclic analogs evaluated, none exhibited similar potency to berberirubine as an inhibitor of topoisomerase ll. Of tbe analogs studied, 2,3-desmethylene-9,10- desmethylberberine was the most potent inhibitor of topoisomerase I when assayed in vitro.File in questo prodotto:
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