某些戊氮杂苊、己氮杂苊及其相应核苷的合成与生物活性。

The synthesis and biological activity of certain pentaazaacenaphthylenes, hexaazaacenaphthylenes and their corresponding nucleosides.

作者信息

Townsend L B, Kawasaki A M, VanSickle A P, Wotring L L

出版信息

Nucleic Acids Symp Ser. 1986(17):41-4.

Abstract

Synthesis of the tricyclic nucleoside 8-amino-6-N-methyl-2-(beta-D-ribo-furanosyl)-1,2,3,5,6,7-hexaazaacena phthylene (5) has been accomplished by the ring closure of an appropriately substituted pyrazolo[3,4-d]-pyrimidine nucleoside followed by the requisite chemical conversions. The formation, isolation and structural elucidation of two unexpected nucleosides formed by a reductive ring cleavage of the hexaazaacenaphthylene ring system is discussed. A comparison of the antitumor and biological activity of 5 with the structurally related tricyclic pentaazaacenaphthylene nucleoside which is currently in phase II clinical trials at the 5'-phosphate pro-drug is also presented.

摘要

通过适当取代的吡唑并[3,4-d]嘧啶核苷的闭环反应，随后进行必要的化学转化，已完成三环核苷8-氨基-6-N-甲基-2-(β-D-呋喃核糖基)-1,2,3,5,6,7-六氮杂并四苯（5）的合成。讨论了由六氮杂并四苯环系统的还原开环反应形成的两种意外核苷的形成、分离和结构解析。还给出了5与目前处于5'-磷酸前药II期临床试验的结构相关三环五氮杂并四苯核苷的抗肿瘤和生物活性比较。

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