Preparation of polyethylene oxide with 4-amino-N-(2-pyrimidinyl) benzene sulfonamide and diethylenetriaminepentaacetic acid end groups and its enrichment in tumour tissues  

作　　者：黄骏廉 陈胜 谈立松 王海原 

出　　处：《Science China Chemistry》1998年第1期54-59,共6页中国科学（化学英文版）

基　　金：ProjectsupportedbytheNationalNaturalScienceFoundationofChina DoctorTrainingFoundationoftheStateEducationCommissionofChinaandtheNaturalScienceFoundationofShanghai

摘　　要：Using polyethylene oxide (PEO) with 4 amino N (2 pyrimidinyl) benzene sulfonamide (APBS) and hydroxyl end groups (PEO a h ) as parent compounds, PEO with diethylenetriaminepentaacetic acid (DTPA) and APBS end groups (PEO a d ) was prepared by functionization of PEO a h . After complexation of PEO a d with isotopes of 153 Sm and 99 Tc, and injecting the polymer drug into the Kunming white mouse transplanted with Sarcoma 180, it was confirmed by γ counter that the PEO a d could be concentrated selectively in the tumour tissues, the ratio of concentration of the polymer drug in tumour tissue to that in ordinary organs such as liver, heart, spleen, muscle, blood and bone marrow is about 2.3:1 or even 10:1.Using polyethylene oxide (PEO) with 4-amino-N-(2-pyrimidinyl) benzene sulfonamide (APBS) and hydroxyl end groups (PEOa-h) as parent compounds, PEO with diethylenetriaminepentaacetic acid (DTPA) and APBS end groups (PEOa-d) was prepared by functionization of PEOa-h. After complexation of PEOa-d with isotopes of153Sm and99Tc, and injecting the polymer drug into the Kunming white mouse transplanted with Sarcoma-180, it was confirmed by γ-counter that the PEOa-d could be concentrated selectively in the tumour tissues, the ratio of concentration of the polymer drug in tumour tissue to that in ordinary organs such as liver, heart, spleen, muscle, blood and bone marrow is about 2.3:1 or even 10:1.

关 键 词：polyethylene oxide 4-amino-N-(2-pyrimidinyl) benzene sulfonamide diethylenetriaminepentaacetic acid anti-turnour drug directing function 

分 类 号：R962[医药卫生—药理学]