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

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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

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    Georg, G. I., Ali, S. M., Boge, T. C., Datta, A., Falborg, L., Park, H., Mejillano, M., & Himes, R. H. (1995). Synthesis of biologically active 2-benzoyl paclitaxel analogues. Bioorganic and Medicinal Chemistry Letters, 5(3), 259-264.