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作为与聚醛葡聚糖结合物的酰肼类药物:合成、表征及稳定性

Hydrazide pharmaceuticals as conjugates to polyaldehyde dextran: syntheses, characterization, and stability.

作者信息

Heindel N D, Zhao H R, Leiby J, VanDongen J M, Lacey C J, Lima D A, Shabsoug B, Buzby J H

机构信息

Institute for Health Sciences and Department of Chemistry, Lehigh University, Bethlehem, Pennsylvania 18015.

出版信息

Bioconjug Chem. 1990 Jan-Feb;1(1):77-82. doi: 10.1021/bc00001a010.

DOI:10.1021/bc00001a010
PMID:1710144
Abstract

The coupling of ellipticine and CI-921, two antineoplastic pharmaceuticals, to polyaldehyde dextran can be carried out under mild reaction conditions with novel acid hydrazides of the parent drugs. The resulting acyl hydrazones resist hydrolytic and enzymatic cleavage and offer a method for drug loading via dextran conjugates to monoclonal antibodies.

摘要

椭圆玫瑰树碱和CI - 921这两种抗肿瘤药物与聚醛葡聚糖的偶联反应,可以在温和的反应条件下,通过母体药物的新型酰肼来实现。所得的酰腙能抵抗水解和酶解,为通过葡聚糖缀合物将药物负载到单克隆抗体上提供了一种方法。

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