Setzer W N, Gu X, Wells E B, Setzer M C, Moriarity D M
Department of Chemistry, University of Alabama in Huntsville, 35899, USA.
Chem Pharm Bull (Tokyo). 2000 Nov;48(11):1776-7. doi: 10.1248/cpb.48.1776.
The synthesis of a series of diacetylenic compounds related to the natural product falcarindiol has been carried out. Unsymmetrical diacetylenes were prepared by a modification of the Cadiot-Chodkiewicz coupling reaction, while a Glaser coupling was used to prepare symmetrical diacetylenes. These compounds have been tested for in vitro cytotoxic activity against Hep-G2, and H-4-II-E cell lines. Diacetylenes with additional unsaturation at C-1, 2, appended with hydroxyl groups at C-3 and C-8, or with long hydrophobic chains, exhibited IC50 values in the micromolar range.
已开展了一系列与天然产物镰叶芹二醇相关的二乙炔类化合物的合成工作。通过改良的卡迪奥特-乔德凯维奇偶联反应制备不对称二乙炔，而采用格拉泽偶联反应制备对称二乙炔。已对这些化合物针对肝癌细胞系Hep-G2和大鼠肝癌细胞系H-4-II-E进行了体外细胞毒性活性测试。在C-1、2位具有额外不饱和键、在C-3和C-8位带有羟基或带有长疏水链的二乙炔，其半数抑制浓度（IC50）值在微摩尔范围内。
