Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group

Effects on HDAC biology and antiproliferative activity

Subhasish Tapadar, Rong He, Doris N. Luchini, Daniel D. Billadeau, Alan P. Kozikowski

Research output: Contribution to journalArticle

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.

Original languageEnglish (US)
Pages (from-to)3023-3026
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number11
DOIs
StatePublished - Jun 1 2009
Externally publishedYes

Fingerprint

Hydroxamic Acids
Isoxazoles
Histone Deacetylase Inhibitors
Chelation
Pancreatic Neoplasms
Assays
Protein Isoforms
Cells
Cell Line

Keywords

  • HDAC
  • HDAC inhibitor
  • Isoform
  • Pancreatic cancer

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry

Cite this

Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group : Effects on HDAC biology and antiproliferative activity. / Tapadar, Subhasish; He, Rong; Luchini, Doris N.; Billadeau, Daniel D.; Kozikowski, Alan P.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 19, No. 11, 01.06.2009, p. 3023-3026.

Research output: Contribution to journalArticle

Tapadar, Subhasish ; He, Rong ; Luchini, Doris N. ; Billadeau, Daniel D. ; Kozikowski, Alan P. / Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group : Effects on HDAC biology and antiproliferative activity. In: Bioorganic and Medicinal Chemistry Letters. 2009 ; Vol. 19, No. 11. pp. 3023-3026.
@article{929897cc2c9f43a88e1b214bd1e7b8b7,
title = "Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: Effects on HDAC biology and antiproliferative activity",
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.",
keywords = "HDAC, HDAC inhibitor, Isoform, Pancreatic cancer",
author = "Subhasish Tapadar and Rong He and Luchini, {Doris N.} and Billadeau, {Daniel D.} and Kozikowski, {Alan P.}",
year = "2009",
month = "6",
day = "1",
doi = "10.1016/j.bmcl.2009.04.058",
language = "English (US)",
volume = "19",
pages = "3023--3026",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier Limited",
number = "11",

}

TY - JOUR

T1 - Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group

T2 - Effects on HDAC biology and antiproliferative activity

AU - Tapadar, Subhasish

AU - He, Rong

AU - Luchini, Doris N.

AU - Billadeau, Daniel D.

AU - Kozikowski, Alan P.

PY - 2009/6/1

Y1 - 2009/6/1

N2 - 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.

AB - 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.

KW - HDAC

KW - HDAC inhibitor

KW - Isoform

KW - Pancreatic cancer

UR - http://www.scopus.com/inward/record.url?scp=65149094611&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=65149094611&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2009.04.058

DO - 10.1016/j.bmcl.2009.04.058

M3 - Article

VL - 19

SP - 3023

EP - 3026

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

IS - 11

ER -