Abstract
A simple synthesis of the β-lactams 11-13 and 16-17 as novel histone deacetylase (HDAC) inhibitors is described. The key synthetic strategies involved the O-alkylation of 6-APA and the coupling reactions of freshly prepared N-carbobenzyloxy-L-prolines 5 and 6 and 6-aminopenicillanates 8-10 and 15 in high yields. It was found that all compounds show potent growth inhibitory activity on human tumor cell lines, the most potent compound 16 exhibiting an IC50 = 2.1 μM in vitro.
Original language | English |
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Pages (from-to) | 1459-1464 |
Number of pages | 6 |
Journal | Zeitschrift fur Naturforschung - Section B Journal of Chemical Sciences |
Volume | 62 |
Issue number | 11 |
DOIs | |
State | Published - Nov 2007 |
Keywords
- Anticancer
- Coupling reaction
- Histone deacetylase
- Synthesis
- β-lactams