杂合产乙酸素、不含α,β-不饱和-γ-内酯的含氮杂环类似物的合成及其对人癌细胞系的细胞毒性。
Synthesis of hybrid acetogenins, alpha,beta-unsaturated-gamma-lactone-free nitrogen-containing heterocyclic analogues, and their cytotoxicity against human cancer cell lines.
作者信息
Kojima Naoto, Fushimi Tetsuya, Maezaki Naoyoshi, Tanaka Tetsuaki, Yamori Takao
机构信息
Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamadaoka, Suita, Osaka 565-0879, Japan.
出版信息
Bioorg Med Chem Lett. 2008 Mar 1;18(5):1637-41. doi: 10.1016/j.bmcl.2008.01.057. Epub 2008 Jan 19.
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.
已合成了一系列天然单四氢呋喃产乙酸菌素索拉明的不含α,β-不饱和-γ-内酯的含氮杂环类似物，并研究了它们对39种肿瘤细胞系的细胞毒性。其中一种，即1-甲基吡唑-5-基衍生物，对NCI-H23细胞显示出细胞毒性的选择性增加，其效力比索拉明高80倍。
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