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Synthetic approaches to the guanosine and xanthosine analogues 5-amino-3-beta-D-ribofuranosylpyrazolo[3,4-e][1,3]oxazin-7-one and 3-beta-D-ribofuranosylpyrazolo[3,4-e][1,3]oxazine-5,7-dione and studies of their antitumor potential.

作者信息

Zou R M, Beylin V G, Groziak M P, Wotring L L, Townsend L B

机构信息

Department of Medicinal Chemistry, College of Pharmacy, University of Michigan, Ann Arbor 48109-1065.

出版信息

J Med Chem. 1991 Jul;34(7):1951-9. doi: 10.1021/jm00111a005.

DOI:10.1021/jm00111a005
PMID:2066967
Abstract

5-Amino-3-beta-D-ribofuranosylpyrazolo[3,4-e][1,3]oxazin-7-o ne has been synthesized via cyclization of the appropriately protected pyrazofurin derivatives and subsequent transformations of the heterocyclic moiety. This guanosine analogue was marginally cytotoxic to L1210 cells in vitro. The xanthosine analogue 3-beta-D-ribofuranosylpyrazolo[3,4-e][1,3]oxazine-5,7-dione was also synthesized, and was found to be highly cytotoxic. It appeared to act as a prodrug of pyrazofurin.

摘要

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