Synthesis of hybrid acetogenins, α,β-unsaturated-γ-lactone-free nitrogen-containing heterocyclic analogues, and their cytotoxicity against human cancer cell lines

Synthesis of hybrid acetogenins, α,β-unsaturated-γ-lactone-free nitrogen-containing heterocyclic analogues, and their cytotoxicity against human cancer cell lines
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DOI:
10.1016/j.bmcl.2008.01.057
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发表时间:
2008-03-01
影响因子:
2.7
通讯作者:
Yamori, Takao
Yamori, Takao
中科院分区:
医学4区
文献类型:
--
作者:
Kojima, Naoto;Fushimi, Tetsuya;Yamori, Takao

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合成了一系列茄素(solamin)的α,β-不饱和-γ-内酯类含氮杂环类似物,并研究了它们对39种肿瘤细胞的细胞毒性。其中1-甲基吡唑-5-基衍生物对NCI-H_(23)的细胞毒活性比茄胺高80倍。(c)2008爱思唯尔有限公司保留所有权利。
A series of alpha,beta-unsaturated-gamma-lactone-free nitrogen-containing heterocyclic analogues of solamin, a natural mono-THF acetogenin, have been synthesized and their cytotoxicity was investigated against 39 tumor cell lines. One of them, 1-methylpyrazol-5-yl derivative, showed selective increase of cytotoxicity against NCI-H23 with 80 times higher potency than solamin. (c) 2008 Elsevier Ltd. All rights reserved.