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Triciribine

Triciribine phosphate is the phosphate ester of the synthetic, cell-permeable tricyclic nucleoside triciribine with potential antineoplastic activity. Triciribine inhibits the phosphorylation, activation, and signalling of Akt-1, -2, and -3, which may result in the inhibition of Akt-expressing tumor cell proliferation. Akts are anti-apoptotic serine/theronine-specific protein kinases that phosphorylate and inactivate components of the apoptotic machinery, including Bcl-xL/Bcl-2-associated death promoter (BAD) and caspase 9. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)

Current developer:   VioQuest Pharmaceuticals Inc。

Synonyms: tricyclic nucleoside 5'-phosphate tricycloside phosphate; Abbreviation: TCN-P; Chemical structure names:

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36: Migawa MT, Drach JC, Townsend LB. Design, synthesis and antiviral activity of novel 4,5-disubstituted 7-(beta-D-ribofuranosyl)pyrrolo[2,3-d][1,2,3]triazines and the novel 3-amino-5-methyl-1-(beta-D-ribofuranosyl)- and 3-amino-5-methyl-1-(2-deoxy-beta-D-ribofuranosyl)-1,5-dihydro-1,4,5,6,7,8-hexaaza acenaphthylene as analogues of triciribine. J Med Chem. 2005 Jun 2;48(11):3840-51. PubMed PMID: 15916436.

37: Smith KL, Lai VC, Prigaro BJ, Ding Y, Gunic E, Girardet JL, Zhong W, Hong Z, Lang S, An H. Synthesis of new 2'-beta-C-methyl related triciribine analogues as anti-HCV agents. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3517-20. PubMed PMID: 15177464.

38: Porcari AR, Townsend LB. An improved total synthesis of triciribine: a tricyclic nucleoside with antineoplastic and antiviral properties. Nucleosides Nucleotides Nucleic Acids. 2004;23(1-2):31-9. PubMed PMID: 15043134.

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41: Gudmundsson KS, Wang Z, Daluge SM, Feldman PL. Synthesis of carbocyclic analogs of 2',3'-dideoxysangivamycin, 2',3'-dideoxytoyocamycin, and 2',3'-dideoxytriciribine. Nucleosides Nucleotides Nucleic Acids. 2001 Oct-Nov;20(10-11):1823-30. PubMed PMID: 11719995.

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