2. Academic Validation
  3. Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: effects on HDAC biology and antiproliferative activity

Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: effects on HDAC biology and antiproliferative activity

  • Bioorg Med Chem Lett. 2009 Jun 1;19(11):3023-6. doi: 10.1016/j.bmcl.2009.04.058.
Subhasish Tapadar 1,  Rong He,  Doris N Luchini,  Daniel D Billadeau,  Alan P Kozikowski
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry & Pharmacognosy, University of Illinois at Chicago, Chicago, IL 60612, USA.
PMID: 19419863 DOI: 10.1016/j.bmcl.2009.04.058
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.

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