Antitumor activity of benzamide riboside in vitro and in vivo.
Benzamide riboside (BR), a recent synthetic nucleoside analogue, is a new compound demonstrating potent cytotoxic activity in malignant cell lines in vitro and in vivo in L1210 leukemia. It exhibits at least two different mechanisms of action. These are, first, the inhibition of inosine 5'-monophosphate dehydrogenase (IMPDH, EC 1.1.1.205), a rate-limiting enzyme for GTP and dGTP synthesis that plays a major role in DNA synthesis, cell proliferation and regulation; and second, the induction of apoptosis. Some aspects of BR activity in malignant cells in vitro and in vivo are reviewed as well as some of the mechanisms behind BR's anti-neoplastic effect.
Novotny
Ladislav
L
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Health Science Center, Kuwait University, Safat. novotny@hsc.kuniv.edu.kw
Rauko
Peter
P
Yalowitz
Joel A
JA
Szekeres
Thomas
T
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D002455:Cell Division / Q000187:drug effects; D004261:DNA Replication / Q000187:drug effects; D005260:Female; D006801:Humans; D007168:IMP Dehydrogenase / Q000037:antagonists & inhibitors*; D066298:In Vitro Techniques; D007939:Leukemia L1210 / Q000188:drug therapy / Q000201:enzymology; D009705:Nucleosides / Q000494:pharmacology*; D010051:Ovarian Neoplasms / Q000188:drug therapy; D019311:Staurosporine / Q000008:administration & dosage; D015996:Survival Rate
D000970:Antineoplastic Agents; D009705:Nucleosides; C076145:3-(1-deoxyribofuranosyl)benzamide; D007168:IMP Dehydrogenase; D019311:Staurosporine