Mellado W, Magri N F, Kingston D G, Garcia-Arenas R, Orr G A, Horwitz S B
Biochem Biophys Res Commun. 1984 Oct 30;124(2):329-36. doi: 10.1016/0006-291x(84)91557-2.
Synthesis and biological activity of 2'-acetyltaxol and 7-acetyltaxol are reported. Activity is measured in vivo by cytotoxicity toward the macrophage-like cell line J774.2, and in vitro by promotion of microtubule assembly in the absence of exogenous GTP. Addition of an acetyl moiety at C-2' results in loss of in vitro activity but not cytotoxicity. The properties of 7-acetyltaxol are similar to those of taxol in its effects on cell replication and on in vitro microtubule polymerization. Therefore a free hydroxyl group at C-7 is not required for in vitro activity and this position is available for structural modifications.
报道了2'-乙酰紫杉醇和7-乙酰紫杉醇的合成及其生物活性。通过对巨噬细胞样细胞系J774.2的细胞毒性在体内测定活性，在体外通过在无外源性鸟苷三磷酸（GTP）的情况下促进微管组装来测定活性。在C-2'位添加一个乙酰基部分会导致体外活性丧失，但不影响细胞毒性。7-乙酰紫杉醇在对细胞复制和体外微管聚合的影响方面，其性质与紫杉醇相似。因此，C-7位的游离羟基对于体外活性不是必需的，并且该位置可用于结构修饰。
