Evaluation of the antitumor activity of 1-(3-C-ethynyl-beta-D-ribofuranosyl) (PJ272), a recent ribonucleoside analogue.

Abstract	The antiproliferative properties of a new ribonucleoside derivative, 1-(3'-C-ethynyl-beta-D-ribofuranosyl)uracil (PJ 272) that we synthesized a few years ago, were investigated in vitro on a variety of tumor cell lines from human and murine origins and in vivo, in tumor bearing mice. Using the 3(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, we showed the ability of this compound to depress, at nanomolar concentrations, the growth of leukemia and lymphoma cultured cells. In 7 out of 8 tumor cell lines tested concentration of 50% inhibition (IC50) was found to be less than 25 nM. PJ 272 was also shown to present the same cytotoxicity against K562 Adriamycin-resistant cell line, which express a multi-drug resistance (MDR) phenotype, and its Adriamycin-sensitive parent cell line. Moreover, when injected intraperitoneally at 20 mg/kg every three days, PJ 272 was found to significantly increase the survival rate (T/C = 149%) of DBA/2 mice injected intraperitoneally with L1210 leukemic cells. Taken together, these results suggest that PJ 272 could be considered as a potentially very active drug against lymphoma and leukemia.
Authors	V Holl, P Jung, D Weltin, J Dauvergne, A Burger, D Coelho, P Dufour, A M Aubertin, P L Bischoff, J F Biellmann
Journal	Anticancer research (Anticancer Res) 2000 May-Jun Vol. 20 Issue 3A Pg. 1739-42 ISSN: 0250-7005 [Print] Greece
PMID	10928102 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References	1-(3-C-ethynylribopentofuranosyl)uracil Antineoplastic Agents Ribonucleosides Uridine
Topics	Animals Antineoplastic Agents (pharmacology, therapeutic use) Cell Division (drug effects) Cell Survival (drug effects) Disease Models, Animal Drug Screening Assays, Antitumor Evaluation Studies as Topic Humans Inhibitory Concentration 50 Jurkat Cells K562 Cells Leukemia L1210 (pathology) Male Mice Mice, Inbred DBA Neoplasm Transplantation Neoplasms, Experimental (drug therapy) Ribonucleosides (pharmacology) Treatment Outcome Tumor Cells, Cultured Uridine (analogs & derivatives, pharmacology, therapeutic use)

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