Synthesis of biologically active 2-benzoyl paclitaxel analogues

Gunda I. Georg, Syed M. Ali, Thomas C. Boge, Apurba Datta, Lise Falborg, Haeil Park, Marisan Mejillano, Richard H. Himes

Research output: Contribution to journalArticlepeer-review

19 Scopus citations


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 (US)
Pages (from-to)259-264
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Issue number3
StatePublished - Feb 2 1995

Bibliographical note

Funding Information:
Financial support from the National Institutes of Health (CA 55141 and CA55100) is acknowledged. The Danish Research Academy ($930093) and Familien Hede Nielsens Fond are acknowledged for grants to Lise Falborg. Support is also acknowledged from the Scientific Education Partnership of Marion Merr¢ll Dow for a postdoctoral fellowship awarded to Thomas C. Boge and from the Kansas Health Foundation for a postdoctoral fellowship awarded to Syed M. AlL We arc grateful for the excellent technical assistance of Ms. Christine


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