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Exploring alternative Zn-binding groups in the design of HDAC inhibitors: squaric acid, N-hydroxyurea, and oxazoline analogues of SAHA.

Authors :
Hanessian S
Vinci V
Auzzas L
Marzi M
Giannini G
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.

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