Abstract
Two novel taxol analogues, baccatin III 13-(N-(p-chlorobenzoyl)-(2′R,3′S)-phenylisoserinate) (2) and baccatin III 13-(N-benzoyl-(2′R,3′S)-3′(p-chlorophenyl)isoserinate) (3) were synthesized from 7-triethylsilyl baccatin III (4) and N-acyl 3-ethoxyethyloxy-4-aryl-2-azetidinones 5 and 6 in two steps and excellent overall yield. Both derivatives demonstrated activity in the microtubule assembly assay and cytotoxicity against B16 melanoma cells comparable to taxol.
Original language | English (US) |
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Pages (from-to) | 295-298 |
Number of pages | 4 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 2 |
Issue number | 4 |
DOIs | |
State | Published - 1992 |
Keywords
- Taxol analogues
- cytotoxicity
- microtubule assembly
- synthesis
- β-lactams