POLYCYCLIC LACTAM DERIVATIVES FOR SENSITIZING MULTIDRUG-RESISTANT CELLS TO ANTITUMOUR AGENTS

摘要

Staurosporin derivatives of formula (I), wherein R1 is formyl, an aliphatic hydrocarbon radical having up to 29 carbon atoms that is unsubstituted or substituted by aryl, or is an aryl radical, R2 is an aliphatic, carbocyclic, carbocyclic-aliphatic, heterocyclic or heterocyclic-aliphatic radical each having up to 29 carbon atoms that is other than C1-C5alkyl, or is a heterocyclic or heterocyclic-aliphatic radical each having up to 20 carbon atoms and up to 9 hetero atoms, or is an acyl radical having up to 30 carbon atoms that is other than benzoyl, benzyloxycarbonyl, lower alkanoyl or alpha -aminoacyl having a free or protected amino group, and R3 is hydrogen, hydroxy, lower alkoxy or oxo, are described. These derivatives can be used for avoiding or removing multidrug resistance to antitumour agents, such as vinblastine or adriamycin.