Cobalt complexes as anticancer agents.

摘要

The invention provides compounds of the general formulae <CHEM> where X and Y separately represent H, lower alkyl (optionally substituted with hydroxy and/or amino functions) containing from 1 to 6 carbon atoms, or phenyl; R represents H, lower alkyl (optionally substituted with hydroxy and/or amino functions) containing from 1 to 6 carbon atoms, phenyl (optionally substituted with Me, OQ, CONHQ and/or NHCOQ, where Q is lower alkyl optionally substituted with hydroxy and/or amino functions and containing from 1 to 6 carbon atoms) or halogen, and Z<-> is Cl<->, Br<->, I<->, ClO4<->, NO3<->, HCO3<-> or any other pharmaceutically-acceptable organic or inorganic counterion, <CHEM> where R1-R5 separately represent H, lower alkyl (optionally substituted with hydroxy and/or amino functions) containing from 1 to 6 carbon atoms, or CH2CH2Cl, except that not more than two of R1-R5 shall represent CH2CH2Cl groups in any one molecule; L1-L3 separately represent all possible combinations of Cl<->, NO2<-> and NH3 monodentate ligands, or a combination of one of these monodentate ligands together with a bidentate ligand (e.g., acetylacetonato), or may collectively represent a tridentate ligand, for example iminodiacetato, N-(Q)iminodiacetato where Q is lower alkyl (optionally substituted with hydroxy and/or amino functions) containing from 1 to 6 carbon atoms, glycylglycinato or 2,6-pyridinedicarboxylato; n is 0 or 1, and, when n = 1, Z<-> represents Cl<->, Br<->, I<->, ClO4<->, NO3<->, HCO3<-> or any other pharmaceutically-acceptable organic or inorganic counterion, and <CHEM> where L1 and L2 together represent two monodentate ligands (e.g., aquo or NH3), or a bidentate ligand, for example ethylenediamine, 1,2-diaminopropane, 1,3-diaminopropane, 2,2 min -bipyridine,o-phenanthroline, or N-(Q)amminoacetato where Q is lower alkyl (optionally substituted with hydroxy and/or amino functions) containing from 1 to 6 carbon atoms; n is 0 or 1, and, when n = 1, Z<-> represents Cl<->, Br<->, I<->, ClO4<->, NO3<->, HCO3<-> or any other pharmaceutically-acceptable organic or inorganic counterion, and processes for their preparation. The compounds have cytotoxic and antitumour activity and are useful as antitumour agents.