SYNTHESIS OF BIOLOGICALLY-ACTIVE 2-BENZOYL PACLITAXEL ANALOGS

GI GEORG*, SM ALI, TC BOGE, A DATTA, L FALBORG, H PARK, M MEJILLANO, RH HIMES

*Corresponding author for this work

Research output: Contribution to journal/Conference contribution in journal/Contribution to newspaperJournal articleResearchpeer-review

Abstract

The influence of aromatic substitution at the 2-benzoyl moiety of paclitaxel 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 against B16 melanoma cells. Most of the analogues were found to possess biological properties similar to paclitaxel.

Original languageEnglish
JournalBioorganic & Medicinal Chemistry Letters
Volume5
Issue3
Pages (from-to)259-264
Number of pages6
ISSN0960-894X
Publication statusPublished - 2 Feb 1995

Keywords

  • TAXOL ANALOGS
  • DRUG DESIGN

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