Synthesis and cytotoxicity study of alkannin derivatives
Synthesis and cytotoxicity study of alkannin derivatives
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阿尔卡宁衍生物的合成及细胞毒性研究
DOI：
10.1016/j.ejmech.2004.05.004
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发表时间：
2004-09-01
影响因子：
6.7
通讯作者：
Li, YM
中科院分区：
文献类型：
--
作者：
Huang, ZS;Wu, HQ;Li, YM
通过β，β-二甲基丙烯酰基紫草素（1）（从新疆紫草（Arnebia euchroma）的根中分离出的最丰富的异己烯基萘唑胺）与不同类型的亲核试剂（如胺和硫醇）在不存在或存在还原剂的情况下反应制备紫草素衍生物（3-19）。发现1-8、10-14和19对四种人癌细胞系（GLC-82、CNE-2、Bel-7402、K-562）的细胞毒性明显高于天然存在的β，β-二甲基丙烯酰紫草素（1）和乙酰紫草素（2）。这项研究也阐明了对紫草素的化学反应性方面的生物活性的理解。(C)2004年，Elsevier SAS。All rights reserved.
Alkannin derivatives (3-19) were prepared through the reaction of beta,beta-dimethylacrylalkannin (1), the most abundant isohexenylnaphthazarm isolated from the roots of Arnebia euchroma, with different types of nucleophiles such as amines and thiols in the absence or presence of a reducing agent. The cytotoxicities of 1-8, 10-14 and 19 against four human carcinoma cell line (GLC-82, CNE2, Bel-7402, K-562) were found to be markedly higher than that of the naturally occurring beta,beta-dimethylacrylalkannin (1) and acetylalkannin (2). This study also shed light on the understanding of the biological activities in terms of the chemical reactivity of alkannins. (C) 2004 Elsevier SAS. All rights reserved.