Orally active docetaxel analogue: Synthesis of 10-deoxy-10-C-morpholinoethyl docetaxel analogues

Authors
Iimura, S Uoto, K Ohsuki, S Chiba, J Yoshino, T Iwahana, M Jimbo, T Terasawa, H Soga, T
Citation
S. Iimura et al., Orally active docetaxel analogue: Synthesis of 10-deoxy-10-C-morpholinoethyl docetaxel analogues, BIOORG MED, 11(3), 2001, pp. 407-410
Citations number
18
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
3
Year of publication
2001
Pages
407 - 410
Database
ISI
SICI code
0960-894X(20010212)11:3<407:OADASO>2.0.ZU;2-H
Abstract
To improve cytotoxicity of 10-deoxy-10-C-morpholinoethyl docetaxel analogue s against various turner cell lines including resistant cells expressing P- glycoprotein (P-gp), we modified the 7-hydroxyl group to hydrophobic groups (methoxy, deoxy, 6,7-olefin, alpha -F, 7-beta -8-beta -methano, fluorometh oxy). Among these analogues. the 7-methoxy analogue showed the strongest cy totoxicity. This analogue showed potent activity against B16 melanoma BL6 i n a vivo by oral administration. (C) 2001 Elsevier Science Ltd. All rights reserved.