Synthesis and biology of 3 '-N-acyl-N-debenzoylpaclitaxel analogues

Authors
Roh, EJ Song, CE Kim, D Pae, HO Chung, HT Lee, KS Chai, KB Lee, CO Choi, SU
Citation
Ej. Roh et al., Synthesis and biology of 3 '-N-acyl-N-debenzoylpaclitaxel analogues, BIO MED CH, 7(9), 1999, pp. 2115-2119
Citations number
23
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY
ISSN journal
09680896 → ACNP
Volume
7
Issue
9
Year of publication
1999
Pages
2115 - 2119
Database
ISI
SICI code
0968-0896(199909)7:9<2115:SABO3'>2.0.ZU;2-Z
Abstract
The 3'-N-acyl-N-debenzoylpaclitaxel analogues 1a-d were synthesized and eva luated on biological systems. Some of the analogues 1a-d exhibited higher c ytotoxicities (up to 20-fold) and stronger abilities to induce apoptosis th an paclitaxel. In an in vivo experiment against ip implanted B16 melanoma, the most cytotoxic compound 1b in vitro caused tumor growth inhibition more than paclitaxel. (C) 1999 Elsevier Science Ltd. All rights reserved.