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3'-C-ethynylcytidine
A synthetic cytidine nucleoside containing a covalently bound ethynyl group with potential antineoplastic and radiosensitizing activities. 3'-C-ethynylcytidine is metabolized in tumor cells to ethynylcytidine triphosphate (ECTP), which inhibits RNA synthesis by competitive inhibition of RNA polymerases I, II and III; subsequently, RNase L is activated, resulting in apoptosis. RNase L is a potent antiviral and antiproliferative endoribonuclease that cleaves singled stranded RNA, causes 28s rRNA fragmentation, and activates Janus Kinase (JAK), a mitochondrial-dependent apoptosis signaling molecule. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)
Abbreviation: | ECyd | ||
Code name: | TAS-106 | ||
Chemical structure: | 1-(3-C-ethynyl-beta-D-ribo-pentofuranosyl)cytosine | ||