Synthesis and biological evaluation of 2-acyl analogues of paclitaxel (Taxol) Academic Article uri icon

Overview

MeSH Major

  • Antineoplastic Agents, Phytogenic
  • Paclitaxel

abstract

  • The anticancer drug paclitaxel (Taxol) has been converted to a large number of 2-debenzoyl-2-aroyl derivatives by three different methods. The bioactivities of the resulting analogues were determined in both tubulin polymerization and cytotoxicity assays, and several analogues with enhanced activity as compared with paclitaxel were discovered. Correlation of cytotoxicity in three cell lines with tubulin polymerization activity showed reasonable agreement. Among the cell lines examined, the closest correlation with antitubulin activity was observed with a human ovarian carcinoma cell line.

publication date

  • September 10, 1998

Research

keywords

  • Academic Article

Identity

Language

  • eng

Digital Object Identifier (DOI)

  • 10.1021/jm980229d

PubMed ID

  • 9733497

Additional Document Info

start page

  • 3715

end page

  • 26

volume

  • 41

number

  • 19