Sapacitabine
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Pyrimidine Antagonist -> Sapacitabine
Sapacitabine Definition
An orally bioavailable pyrimidine analogue prodrug with potential antineoplastic activity. Sapacitabine is hydrolyzed by amidases to the deoxycytosine analogue CNDAC (2'-Cyano-2'-deoxyarabinofuranosylcytosine), which is then phosphorylated into the active triphosphate form. As an analogue of deoxycytidine triphosphate, CNDAC triphosphate incorporates into DNA strands during replication, resulting in single-stranded DNA breaks during polymerization due to beta-elimination during the fidelity checkpoint process; cell cycle arrest in the G2 phase and apoptosis ensue. The unmetabolized prodrug may exhibit antineoplastic activity as well.
Sapacitabine Synonyms
Sapacitabine, CS-682, CYC682, N-[1-(2-Cyano-2-deoxy-beta-D-arabinofuranosyl]-2-oxo-1,2-dihydropyrimidin-4-yl}hexadecanamide
Terms in Sapacitabine category
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