NITROSOUREAS Chemische Eigenschaften,Einsatz,Produktion Methoden
Allgemeine Beschreibung
The nitrosoureas were discovered as a result of drug screeningby the Cancer Chemotherapy National Service Center,which identified N-methyl-N'-nitroguanidine as having activityagainst L1210 leukemia.Further development ofthis lead compound was based on the idea that its chemicaldecomposition was leading to the formation of diazomethane(CH
2N
2) and subsequent alkylation of DNA.This led to the nitrosoureas, where it was found that activitycould be enhanced by attachment of a 2-haloethyl substituentto both nitrogens.
Procarbazine is an antineoplastic agent that was originallydeveloped as a result of efforts to find new inhibitors ofmonoamine oxidase. Subsequent screening revealed antineoplasticactivity.
Hydrazines are also capable of inhibitingmonoamine oxidase as seen with isocarboxazid andphenelzine; however, procarbazine is only a weak inhibitorof this enzyme. The agent is also capable of inhibitingaldehyde dehydrogenase and producing a disulfiram-likereaction. Given the involvement of the CYP system in itsactivation, the action of procarbazine is subject to drug interactionswith both inducers and inhibitors of this system.Somewhat related is dacarbazine, which was initiallythought to act as an inhibitor of purine biosynthesis, but latterwas shown to be an alkylating agent.
NITROSOUREAS Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte