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Exploring alternative Zn-binding groups in the design of HDAC inhibitors: squaric acid, N-hydroxyurea, and oxazoline analogues of SAHA.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2006 Sep 15; Vol. 16 (18), pp. 4784-7. Date of Electronic Publication: 2006 Jul 25. - Publication Year :
- 2006
-
Abstract
- Analogues of suberoylanilide hydroxamic acid (SAHA) were prepared by replacing the Zn-binding group with squaric acid, N-hydroxyurea, and 4-hydroxymethyl oxazoline units, also varying the length of the aliphatic chain. No inhibitory activity on HDAC was observed below 1.0 microM and no cytotoxic activity on different tumor cell lines was seen below 20.0 microM.
- Subjects :
- Drug Design
Enzyme Inhibitors chemistry
Enzyme Inhibitors pharmacology
Histone Deacetylases metabolism
Hydroxamic Acids chemical synthesis
Hydroxamic Acids pharmacology
Molecular Structure
Vorinostat
Alkynes chemistry
Cyclobutanes chemistry
Enzyme Inhibitors chemical synthesis
Histone Deacetylase Inhibitors
Hydroxamic Acids chemistry
Hydroxyurea chemistry
Oxazoles chemistry
Zinc chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 16
- Issue :
- 18
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 16870438
- Full Text :
- https://doi.org/10.1016/j.bmcl.2006.06.090