Synthesis and antitumor activity of cholest-4α-methyl-7-en-3β-ol derivatives
Synthesis and antitumor activity of cholest-4α-methyl-7-en-3β-ol derivatives
复制标题
cholest-4α-甲基-7-en-3β-ol 衍生物的合成和抗肿瘤活性
DOI：
10.1016/j.steroids.2006.01.006
复制
发表时间：
2006-06-01
期刊：
影响因子：
2.7
通讯作者：
Pei, Qiang
中科院分区：
文献类型：
--
作者：
He, Lan;Liu, Yumei;Pei, Qiang
胆甾-4 α-甲基-7-烯-3 β-醇（1）对pc 12肿瘤具有有效的抑制活性，比率为0.5043（10 μ g/mL）。本文介绍了对该化合物进行的一系列结构修饰，重点是3 β-羟基和7（8）-双键的修饰。对人癌细胞系包括结肠癌（HCT-8）、肝癌（BEL-7402）和鼻咽癌（KB）细胞测试了I的合成衍生物。结果表明，胆甾-4 α-甲基-8-烯-3 β，7 α-二醇6a对KB细胞有明显的抑制作用，IC_（50）为1.32 × 10 ~（-9）μ g/ml。此外，该化合物对HCT-8和BEL-7402的细胞毒性特性优异，IC 50为1.2 μ g/mL。(c)2006年爱思唯尔公司All rights reserved.
Cholest-4 alpha-methyl-7-en-3 beta-ol (1) has potent inhibitory activity against pc 12 tumor with 0.5043 ratio (10 mu g/mL). This paper describes a series of structural modification of this compound, which focus on 3 beta-hydroxyl group and 7(8)-double bond. The synthesized derivatives of I were tested for human cancer cell lines including colon cancer (HCT-8), liver cancer (BEL-7402) and nasopharyngeal cancer (KB) cells. The results showed that cholest-4 alpha-methyl-8-en-3 beta,7 alpha-diol 6a inhibits KB cell significantly with IC50 1.32 x 10(-9) mu g/ml. In addition, the cytotoxic properties of this compound against HCT-8 and BEL-7402 are excellent with IC50 1.2 mu g/mL. (c) 2006 Elsevier Inc. All rights reserved.