574-77-6Relevant articles and documents
Protoberberine Alkaloids and Related Compounds as Dual Inhibitors of Mammalian Topoisomerase I and II
Makhey, Darshan,Gatto, Barbara,Yu, Chiang,Liu, Angela,Liu, Leroy F.,LaVoie, Edmond J.
, p. 1 - 12 (2007/10/03)
Berberine and several structurally-related analogs were evaluated as inhibitors of topoisomerase I and II. 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 II. Among the bicyclic heterocyclic analogs evaluated, none exhibited similar potency to berberrubine as an inhibitor of topoisomerase II. Of the analogs studied, 2,3-desmethylene-9,10-desmethylberberine was the most potent inhibitor of topoisomerase I when assayed in vitro.