Background:

Triapine is a potent inhibitor of ribonucleotide reductase activity with IC50 value of 1.6 μM for various of tumor cell lines [1].

Triapine has been reported to inhibit ribonucleotide reductase activity. Triapine has shown its antineoplastic activity by inhibiting DNA synthesis and repair. In addition, Triapine has been revealed to?inhibit the growth of the murine M109 lung carcinoma and human A2780 ovarian carcinoma xenografts in nude mice. Moreover, Triapine was active against the L1210 leukemia over a broad range of dosages and was curative for the M109 lung carcinoma and human A2780 ovarian carcinoma xenograft mice. [1, 2]

参考文献:
[1]. Jennifer J. Knox, Sebastien J. Hotte, Christian Kollmannsberger, Eric Winquist, Bryn Fisher, Elizabeth A. Eisenhauer .Phase II study of Triapine? in patients with metastatic renal cell carcinoma: a trial of the National Cancer Institute of Canada Clinical Trials Group (NCIC IND.161). nvestigational New Drugs .October 2007, Volume 25, Issue 5, pp 471-477
[2]Finch RA1, Liu M, Grill SP, Rose WC, Loomis R, Vasquez KM, Cheng Y, Sartorelli AC. Triapine (3-aminopyridine-2-carboxaldehyde- thiosemicarbazone): A potent inhibitor of ribonucleotide reductase activity with broad spectrum antitumor activity. Biochem Pharmacol. 2000 Apr 15;59(8):983-91