SYNTHESIS OF BIOLOGICALLY-ACTIVE 2-BENZOYL PACLITAXEL ANALOGS

Authors
GEORG GI ALI SM BOGE TC DATTA A FALBORG L PARK H MEJILLANO M HIMES RH
Citation
Gi. Georg et al., SYNTHESIS OF BIOLOGICALLY-ACTIVE 2-BENZOYL PACLITAXEL ANALOGS, Bioorganic & medicinal chemistry letters, 5(3), 1995, pp. 259-264
Citations number
21
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
3
Year of publication
1995
Pages
259 - 264
Database
ISI
SICI code
0960-894X(1995)5:3<259:SOB2PA>2.0.ZU;2-M
Abstract
The influence of aromatic substitution at the 2-benzoyl moiety of pacl itaxel on biological activity was investigated, following the Topliss Operational Scheme. Twelve paclitaxel derivatives were synthesized and evaluated in a microtubule assembly assay and for cytotoxicity agains t B16 melanoma cells. Most of the analogues were found to possess biol ogical properties similar to paclitaxel.