Zheng H, Tong X H, Mao F, Weng L L
School of Pharmacy, West China University of Medical Sciences, Chengdu.
Yao Xue Xue Bao. 1991;26(5):336-40.
Estradiol conjugate has been used as a tracer to detect estrogen receptor of human mammary cancer cells. In order to look for more stable carrier of fluorescent estradiol conjugate, we substituted polyethyleneglycol (PEG) for bovine serum albumin (BSA) and synthsized 17 beta-estradiol-6-carboxymethyl-oxime-PEG-fluorescein isothiocyanate. The structure of the title compound was confirmed by IR and UV. In this paper, we also describe another procedure to convert the terminal hydroxyl groups of PEG to the more reactive primary amino PEG by tosylation, azide group substitution and catalytic hydrogenation. The ratio of conversion is about 87%.
雌二醇缀合物已被用作检测人乳腺癌细胞雌激素受体的示踪剂。为了寻找更稳定的荧光雌二醇缀合物载体，我们用聚乙二醇（PEG）替代牛血清白蛋白（BSA），合成了17β-雌二醇-6-羧甲基肟-PEG-异硫氰酸荧光素。通过红外光谱和紫外光谱对目标化合物的结构进行了确证。本文还描述了另一种方法，通过甲苯磺酰化、叠氮基取代和催化氢化将PEG的末端羟基转化为反应活性更高的伯氨基PEG。转化比例约为87%。
