Synthesis of new dihydropyrazines with DNA strand-breakage activity

Synthesis of new dihydropyrazines with DNA strand-breakage activity
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DOI:
10.1248/cpb.53.1359
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发表时间:
2005-10-01
影响因子:
1.7
通讯作者:
Yamaguchi, T
Yamaguchi, T
中科院分区:
医学4区
文献类型:
--
作者:
Maruoka, H;Kashige, N;Yamaguchi, T

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用 1,2-二胺处理 1,2-环己二酮,例如乙二胺与顺式(和反式)1,2-二氨基环己烷发生[4+2]环缩合,得到相应的二氢吡嗪衍生物(化合物1-6)。它们表现出比二氢吡嗪更强的 DNA 链断裂活性,这在之前的论文中已经报道过。
Treatment of 1,2-cyclohexanedione with 1,2-diamines, e.g. ethylenediamine and cis-(and trans-)1,2-diaminocyclohexane, caused [4+2] cyclocondensation to give the corresponding dihydropyrazine derivatives (compounds 1-6). They exhibited stronger DNA strand-breakage activity than that of dihydropyrazines, which has already been reported in previous papers.