A study of microsomal oxidative functions with the aid of a series of N-colchiceyl derivatives.
N-Colchiceyl derivatives are presented as a class of substances which, provided certain structural requirements are met, are oxidatively degraded by microsomal suspensions both at the nitrogen-linked side chain at ring C and at the oxygen-linked side chain(s) at Ring A. The chemical structures of unknown metabolites have been elucidated by comparison with authentic samples whose syntheses are described. Comparative studies indicate structure-dependent preferred sites for the introduction fo oxygen, whose extent correlates rather closely with the partition coefficient in the system n-octanol/ethanol/water. The results demonstrate, with the inclusion of some inhibition data, the suitability of N-colchiceyl derivatives for detailed investigations of microsomal degradative processes.
D000818:Animals; D003078:Colchicine; D006224:Cricetinae; D005260:Female; D008297:Male; D008862:Microsomes, Liver / Q000201:enzymology*; D006899:Mixed Function Oxygenases / Q000378:metabolism*; D010088:Oxidoreductases / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
D006899:Mixed Function Oxygenases; D010088:Oxidoreductases; D003078:Colchicine