Synthesis and evaluation of Taxol-folic acid conjugates as targeted antineoplastics

Jae Wook Lee, June Y. Lu, Philip Low, P. L. Fuchs

Research output: Contribution to journalArticle

107 Scopus citations

Abstract

A series of Taxol derivatives tethered at C2′ and C-7 to glutamate and folate have been synthesized for evaluation as prodrugs which release Taxol via hydrolytic lability of their α-alkoxy and α-amino esters. The half-time for hydrolysis of these materials was determined in pH 7 and pH 5 buffer. The in vitro cytotoxicity has been assessed in cell culture against A-549 lung cancer, MCF-7 breast cancer, and HT-29 colon cancer. Selected agents were further screened for folate binding and competitive binding with free folic acid. One agent (54), further evaluated in animal studies was found to increase the lifespan in mice, but was less effective than Taxol itself.

Original languageEnglish (US)
Pages (from-to)2397-2414
Number of pages18
JournalBioorganic and Medicinal Chemistry
Volume10
Issue number7
DOIs
StatePublished - May 8 2002

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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