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Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: effects on HDAC biology and antiproliferative activity.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2009 Jun 01; Vol. 19 (11), pp. 3023-6. Date of Electronic Publication: 2009 Apr 20. - Publication Year :
- 2009
-
Abstract
- A series of hydroxamic acid based histone deacetylase inhibitors 6-15, containing an isoxazole moiety adjacent to the Zn-chelating hydroxamic acid, is reported herein. Some of these compounds showed nanomolar activity in the HDAC isoform inhibitory assay and exhibited micro molar inhibitory activity against five pancreatic cancer cell lines.
- Subjects :
- Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Cell Line, Tumor
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors chemistry
Histone Deacetylases metabolism
Humans
Hydroxamic Acids chemical synthesis
Hydroxamic Acids chemistry
Isoxazoles chemical synthesis
Isoxazoles chemistry
Zinc chemistry
Antineoplastic Agents pharmacology
Enzyme Inhibitors pharmacology
Histone Deacetylase Inhibitors
Hydroxamic Acids pharmacology
Isoxazoles pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 19
- Issue :
- 11
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 19419863
- Full Text :
- https://doi.org/10.1016/j.bmcl.2009.04.058