阿霉素的新型腙衍生物及其免疫缀合物——酸稳定性与细胞毒性之间的相关性
New hydrazone derivatives of adriamycin and their immunoconjugates--a correlation between acid stability and cytotoxicity.
作者信息
Kaneko T, Willner D, Monkovíc I, Knipe J O, Braslawsky G R, Greenfield R S, Vyas D M
机构信息
Bristol-Myers Squibb Company, Wallingford, Connecticut 06492-7660.
出版信息
Bioconjug Chem. 1991 May-Jun;2(3):133-41. doi: 10.1021/bc00009a001.
PMID:1932212
Abstract
New N-substituted hydrazine linkers were synthesized and their hydrazone derivatives of adriamycin were prepared. These functionalized adriamycin derivatives were conjugated with a monoclonal antibody, 5E9. The release rate of adriamycin from the hydrazones and from some of the conjugates was studied, and their relationship to the IC50's of the conjugate against 5E9-positive Daudi cells was investigated.
摘要
合成了新型N-取代肼连接体，并制备了其阿霉素腙衍生物。这些功能化的阿霉素衍生物与单克隆抗体5E9偶联。研究了阿霉素从腙以及一些偶联物中的释放速率，并研究了它们与偶联物对5E9阳性Daudi细胞的IC50值之间的关系。
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