Synthesis of paclitaxel-BGL conjugates.
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.
Department of Pharmaceutical Chemistry, Institute of Health Biosciences, Graduate School of The University of Tokushima, 1-78, Sho-machi, Tokushima 770-8505, Japan. nem@ph.tokushima-u.ac.jp
Hisao
H
Nemoto
Ayato
A
Katagiri
Masaki
M
Kamiya
Tomoyuki
T
Kawamura
Tsuyoshi
T
Matsushita
Kosuke
K
Matsumura
Tomohiro
T
Itou
Hatsuhiko
H
Hattori
Miho
M
Tamaki
Keisuke
K
Ishizawa
Licht
L
Miyamoto
Shinji
S
Abe
Koichiro
K
Tsuchiya
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004305:Dose-Response Relationship, Drug; D005990:Glycerol / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D008968:Molecular Conformation; D008970:Molecular Weight; D009374:Neoplasms, Experimental / Q000188:drug therapy*; D017239:Paclitaxel / Q000737:chemistry* / Q000494:pharmacology*; D012995:Solubility; D013329:Structure-Activity Relationship; D023041:Xenograft Model Antitumor Assays
D000972:Antineoplastic Agents, Phytogenic; D017239:Paclitaxel; D005990:Glycerol