Synthesis of Paclitaxel-BGL Conjugates

被引:10
|
作者
Nemoto, Hisao [1 ]
Katagiri, Ayato [1 ]
Kamiya, Masaki [1 ]
Kawamura, Tomoyuki [1 ]
Matsushita, Tsuyoshi [1 ]
Matsumura, Kosuke [1 ]
Itou, Tomohiro [1 ]
Hattori, Hatsuhiko [1 ]
Tamaki, Miho [2 ]
Ishizawa, Keisuke [2 ]
Miyamoto, Licht [2 ]
Abe, Shinji
Tsuchiya, Koichiro [2 ]
机构
[1] Univ Tokushima, Grad Sch, Inst Hlth Biosci, Dept Pharmaceut Chem, Tokushima 7708505, Japan
[2] Univ Tokushima, Grad Sch, Inst Hlth Biosci, Dept Med Pharmacol, Tokushima 7708505, Japan
基金
日本科学技术振兴机构;
关键词
Water-solubility; Paclitaxel; Glycerol; Anti-tumor agent; Symmetrically branched oligoglycerols; BRANCHED OLIGOGLYCEROL; P-BORONOPHENYLALANINE; CASCADE-TYPE; WATER; DERIVATIVES; BEARING; SOLUBILITY; CARBORANE; TAXOL;
D O I
10.1016/j.bmc.2012.07.031
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Four kinds of symmetrically branched oligoglyceryl trimeric (BGL003)-paclitaxel conjugates and a corresponding heptameric (BGL007) conjugate were synthesized. Molecular weights of all the compounds were less than two times that of paclitaxel. The anti-tumor activity of the most water-soluble BGL003 conjugate was examined and found to be preserved in spite of the chemical modification that is displacement of the N3'-debenzoyl residue with the BGL003 succinyl residue. (C) 2012 Elsevier Ltd. All rights reserved.
引用
收藏
页码:5559 / 5567
页数:9
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