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3-脱氮鸟嘌呤阿拉伯呋喃糖基衍生物的合成

Synthesis of arabinofuranosyl derivatives of 3-deazaguanine.

作者信息

Poonian M S, McComas W W, Kramer M J

出版信息

J Med Chem. 1979 Aug;22(8):958-62. doi: 10.1021/jm00194a014.

DOI:10.1021/jm00194a014
PMID:490540
Abstract

Synthesis of four arabinofuranosyl derivatives of the antitumor agent 3-deazaguanine is described. By the use of 13C and 1H nuclear magnetic resonance spectroscopy, the structures of these nucleosides were established to be alpha and beta pairs of N-7 and N-9 arabinosides of 3-deazaguanine. In contrast to 3-deazaguanine and its ribosyl derivative, the nucleosides described in this paper were found to be inactive against Sarcoma 180 in mice at 100 mg/kg.

摘要

描述了抗肿瘤剂3-脱氮鸟嘌呤的四种阿拉伯呋喃糖基衍生物的合成。通过使用碳-13和氢-1核磁共振光谱，确定这些核苷的结构为3-脱氮鸟嘌呤的N-7和N-9阿拉伯糖苷的α和β对。与3-脱氮鸟嘌呤及其核糖基衍生物相反，本文所述的核苷在100mg/kg剂量下对小鼠肉瘤180无活性。

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