Antimitotic agents: synthesis of imidazo[4,5-c]pyridin-6-ylcarbamates and imidazo[4,5-b]pyridin-5-ylcarbamates.
Antimitotic agents: synthesis of imidazo[4,5-c]pyridin-6-ylcarbamates and imidazo[4,5-b]pyridin-5-ylcarbamates.
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抗有丝分裂剂：咪唑并[4,5-c]吡啶-6-基氨基甲酸酯和咪唑并[4,5-b]吡啶-5-基氨基甲酸酯的合成。
DOI：
10.1021/jm00164a030
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发表时间：
1990
影响因子：
7.3
通讯作者：
TempleJr,C
中科院分区：
文献类型：
--
作者：
TempleJr,C
6]吡嗪类化合物（1）也显示出抗癌活性。1-3 1的1，2-NHCH部分是不稳定的，并且氧化提供无活性的杂芳族化合物。在以前的论文中，我们报道了一些2-芳基-1H-咪唑并[4，5-c]吡啶-6-基氨基甲酸酯（例如，2）作为1的更稳定的环类似物的合成（图I）。虽然1中活性所必需的许多结构特征被结合到2中，但咪唑并吡啶仅显示出最小的活性。较低的活性归因于在环NH基团处缺乏碱性，并且可能归因于1和2的芳基的取向的差异。本文报道了2-位被较灵活的苄硫基取代的1-氨基-咪唑并[4，5-c]吡啶的合成。同时，本工作还提供了一些新的咪唑并[4，5-61-吡啶]环体系的衍生物。
6] pyrazines (1), also have shown anticancer activity. 1-3 The 1, 2-NHCH moiety of 1 is unstable and oxidation provides inactive heteroaromatic compounds. In a previous paper we reported the synthesis of some 2-aryl-1H-imidazo [4, 5-c] pyridin-6-ylcarbamates (eg, 2) as more stable ring analogues of 1 (Chart I). 1 234* Although many of the structural featuresnecessary for activity in 1 were incorporated in 2, the imidazopyridines showed only minimal activity. The lower activity was attributed to the lack of basicity at the ring NH group, and possibly to the differences in orientation of the aryl groups of 1 and 2. In this paper we report the preparation of 1-amino-lii-imidazo [4, 5-c] pyridines substituted at the 2-position with the more flexible benzylthio moiety. Also, this work provided some new derivatives of the imidazo [4, 5-61-pyridine ring system.