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Synthesis and antitumor activity of 2-. beta. -D-ribofuranosylselenazole-4-carboxamide and related derivatives

Journal Article · · J. Med. Chem.; (United States)
DOI:https://doi.org/10.1021/jm00357a024· OSTI ID:5312519
Treatment of 2,3,5-tri-O-benzoyl-..beta..-D-ribofuranosyl-1-carbonitrile with hydrogen selenide provided 2,5-anhydro-3,4,6-tri-O-benzoyl-D-allonselenoamide (3). Compound 3 was treated with ethyl bromopyruvate to provide ethyl 2-(2,3,5-tri-O-benzoyl-D-ribofuranosyl)selenazole-4-carboxylates, which after ammonolysis were converted to 2-..beta..-D-ribofuranosylselenazole-4-carboxamide (6) and its ..cap alpha..-analogue 7, respectively. Acetylation of nucleoside 6 provided 2-(2,3,5-tri-O-acetyl-..beta..-D-ribofuranosyl)selenazole-4-carboxamide, and phosphorylation of 6 provided the corresponding 5'-phosphate 9. Compounds 6 and 9 were found to be cytotoxic toward P388 and L1210 cells in culture and effective against Lewis lung carcinoma in mice.
Research Organization:
Oak Ridge National Lab., TN
OSTI ID:
5312519
Journal Information:
J. Med. Chem.; (United States), Journal Name: J. Med. Chem.; (United States) Vol. 26:3; ISSN JMCMA
Country of Publication:
United States
Language:
English