Benzo[b]thiophene-based histone deacetylase inhibitors

David J. Witter; Sandro Belvedere; Liqiang Chen; J. Paul Secrist; Ralph T. Mosley; Thomas A. Miller

doi:10.1016/j.bmcl.2007.05.091

Benzo[b]thiophene-based histone deacetylase inhibitors

David J. Witter, Sandro Belvedere, Liqiang Chen, J. Paul Secrist, Ralph T. Mosley, Thomas A. Miller

Center for Drug Design

Research output: Contribution to journal › Article › peer-review

41 Scopus citations

Abstract

Benzo[b]thienyl hydroxamic acids, a novel class of histone deacetylase (HDAC) inhibitors, were identified via a targeted screen of small molecule hydroxamic acids. Various substitutions were explored in the C5- and C6-positions of the benzo[b]thiophene core to characterize SAR and develop optimal inhibitors. It was determined that substitution at the C6-position of the benzo[b]thiophene core with a three-atom spacer yielded optimal HDAC1 inhibition and anti-proliferative activity in murine erythroleukemia (SC-9) cells.

Original language	English (US)
Pages (from-to)	4562-4567
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	17
Issue number	16
DOIs	https://doi.org/10.1016/j.bmcl.2007.05.091
State	Published - Aug 15 2007

Bibliographical note

Copyright:
Copyright 2009 Elsevier B.V., All rights reserved.

Keywords

Anticancer drug
Benzo[b]thiophene
HDAC
HDAC inhibitor
Histone deacetylase inhibitor
Hydroxamic acids
SAHA

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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title = "Benzo[b]thiophene-based histone deacetylase inhibitors",

abstract = "Benzo[b]thienyl hydroxamic acids, a novel class of histone deacetylase (HDAC) inhibitors, were identified via a targeted screen of small molecule hydroxamic acids. Various substitutions were explored in the C5- and C6-positions of the benzo[b]thiophene core to characterize SAR and develop optimal inhibitors. It was determined that substitution at the C6-position of the benzo[b]thiophene core with a three-atom spacer yielded optimal HDAC1 inhibition and anti-proliferative activity in murine erythroleukemia (SC-9) cells.",

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AU - Witter, David J.

AU - Belvedere, Sandro

AU - Chen, Liqiang

AU - Secrist, J. Paul

AU - Mosley, Ralph T.

AU - Miller, Thomas A.

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Benzo[b]thiophene-based histone deacetylase inhibitors

Abstract

Bibliographical note

Keywords

UN SDGs

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