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

doi:10.1016/j.bmcl.2009.04.058

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 journal › Article › peer-review

31 Scopus citations

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 language	English (US)
Pages (from-to)	3023-3026
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	19
Issue number	11
DOIs	https://doi.org/10.1016/j.bmcl.2009.04.058
State	Published - Jun 1 2009
Externally published	Yes

Keywords

HDAC
HDAC inhibitor
Isoform
Pancreatic cancer

ASJC Scopus subject areas

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

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10.1016/j.bmcl.2009.04.058

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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.}",

note = "Funding Information: This work was supported in part by gift funds from an anonymous donor, by a Grant (No. 271210) from the ADDF/Elan, and by the Mayo Foundation and the Pancreatic Cancer SPORE P50 CA102701.",

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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.

N1 - Funding Information: This work was supported in part by gift funds from an anonymous donor, by a Grant (No. 271210) from the ADDF/Elan, and by the Mayo Foundation and the Pancreatic Cancer SPORE P50 CA102701.

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

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JO - Bioorganic and Medicinal Chemistry Letters

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IS - 11

ER -

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

Abstract

Keywords

ASJC Scopus subject areas

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