Deletion of the oxetane ring in docetaxel analogues: synthesis and biological evaluation |
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Authors: | Deka Vaishali Dubois Joëlle Thoret Sylviane Guéritte Françoise Guénard Daniel |
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Institution: | Institut de Chimie des Substances Naturelles, CNRS, 91198 Gif-sur-Yvette Cedex, France. |
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Abstract: | Two new docetaxel analogues have been prepared starting from 10-deacetylbaccatin III. Both derivatives lack the oxetane D-ring but possess the 4alpha-acetoxy group, which is important for biological activity. The influence of a more or less constrained C-ring was evaluated by adding, or not adding, a double bond in this ring. Both compounds were found to be equally less active than docetaxel in biological assays. reaction: see text] |
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