Abstract
Objective: To synthesize the anticancer agent combretastatin A-4 and its water-soluble analogues. Methods: 3,4,5-Trimethoxyphenylacetic acid and isovanilline were used as starting materials to prepare combretastatin A-4 and its water-soluble analogues via condensation, modification with mPEG side chain, and de-carboxylation reactions. Results: The structures of target compounds were confirmed by 1H NMR, 13C NMR, MS and melting point; the overall yields were about 40%. Conclusion: The synthetic routes developed herein require simple reaction conditions and few steps, and yield high stereoselectivity of cis conformation, which are suitable for large-scale manufacturing.
Original language | English |
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Pages (from-to) | 1322-1325 |
Number of pages | 4 |
Journal | Chinese Journal of New Drugs |
Volume | 17 |
Issue number | 15 |
Publication status | Published - 2008 |
Externally published | Yes |
Keywords
- Anticancer
- Combretastatin A-4
- Synthesis
- Water-soluble analogues