三尖杉酯碱类似物的合成及其抗肿瘤活性

SYNTHESIS OF ANALOGS OF CEPHALOTAXINE ESTERS AND THEIR ANTITUMOR ACTIVITIES.

摘要: 合成了新结构类型的三尖杉酯碱类似物C₁Z,C₂E,C₃E,C₄E,考察了侧链烯酯酸B₁,B₂,B₃,B₄形成时顺、反异构体的比例,发现顺式构型在酸催化下易转化成反式构型。C₁E对肿瘤细胞HL-60有明显的分化诱导作用及对白血病L₁₂₁₀有抑制作用。

Abstract: Four analogs, of cephalotaxine, esters: (C₁ Z, C₂ E, C₃E, C₄E) were synthesized. The ratio of the, Z, E isomers of the side chain α, β-unsaturated ester carboxylic acids is reported. The Z isomer was easy to transform to the E isomer.Compound C₁Z showed significant activity of inducing cancer cell HL-60 differentiation. It also showed inhibitory activity on Leukemia L₁₂₁₀.