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 |
|---|---|
| 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 |
Bibliographical note
Funding Information:This work has been supported by the KOSEF Brain Neurobiology Grant (2007), by the Ewha Global Challenge (BK21) grant, and in part by Cooperative Agreement Number 1-U01 C1000211 from the Centers for Disease Control and Prevention (M. A. A.).
Keywords
- Anticancer
- Coupling reaction
- Histone deacetylase
- Synthesis
- β-lactams
Fingerprint
Dive into the research topics of 'Synthesis of new β-lactam analogs and evaluation of their histone deacetylase (HDAC) activity'. Together they form a unique fingerprint.Cite this
- APA
- Author
- BIBTEX
- Harvard
- Standard
- RIS
- Vancouver