Synthesis and biological activity of 14-hydroxydocetaxel

Bioorganic & Medicinal Chemistry Letters
1994.0

Abstract

New taxoids, 14β-hydroxydocetaxel and its 1,14-acetonide, are synthesized from 14β-hydroxy-10deacetylbaccatin III in good yields. The cytotoxicity of the new taxoids are evaluated against different human tumor cell lines and their ability to inhibit the microtubules disassembly examined. 14β-hydroxydocetaxel shows very strong cytotoxicity, especially against A549 human non-small cell lung cancer cell line $(IC_{50} = 0.8 ext{ nM})$ .

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