Synthesis and bioactivities of paclitaxel analogs with a cyclopropanated side-chain |
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| Authors: | Changhui LiuMarkus Tamm Marcus W NötzelArmin de Meijere Jennifer K SchillingDavid GI Kingston |
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| Institution: | a Department of Chemistry, M/C 0212, Virginia Polytechnic Institute and State University, Blacksburg, VA 24061, USA
b Institut für Organische Chemie der Georg-August-Universität Göttingen, Tammannstrasse 2, D-37077 Göttingen, Germany |
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| Abstract: | Four paclitaxel analogs with a cyclopropanated side-chain were synthesized by coupling of the spirocyclopropanated oxazoline-5-carboxylic acid 4 with 7-TES-baccatin III, followed by hydrolytic ring opening and rearrangement. The absolute configuration of the 2′-position was determined by NMR analysis of the corresponding Mosher esters. The two new paclitaxel analogs with the R configuration at C-2′ were both active in the A2780 mammalian cell line cytotoxicity assay, but much less than paclitaxel itself. |
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