Ebediynes

Pregunta	Respuesta
Name two drugs that are enediyne	Chalicheamicin and esperamycin are drugs which are enediynes
Mode of action	Formation of a benzenedyl diradical which cleaves a H off central C of DNA and causing eventual DNA cutting and death
Mechanism 1st part	Cellular nucleophile attacks the trigger (trisulphide moiety) 's-sME' bond and forms internal sulphur nucleophile. Then s- undergoes conjugate addition to enone. New bond formed. ketone is reformed as dB takes a H from surrounding. The new bond that formed causes the alkyne bonds to come closer 3.35-3.16A. Allowing Bergmann cyclo aromatisation.
Bergmann cyclo aromatisation	Radical arrows open up the alkyne and formation of a sigma bond formed a 6 MEMBERED cyclo diradical.
DNA Cleavage	Diradical cleaves H Central C radical formed O2 +h radical sees formation of peroxide on central C Reduction sees formation of alcohol The DNA is cleaved forming an aldehyde DNA has successfully been cut and cell dies

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	Creado por ashrafali hace casi 9 años