Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.

doi:10.1016/j.bmcl.2006.10.045

Paper

Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.

Published 2007 · Steve Price, W. Bordogna, R. Braganza

Bioorganic & medicinal chemistry letters

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6

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1

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Abstract

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In Vitro Study

Study Snapshot

Substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids show potential as potent HDAC inhibitors with improved potency, in vitro DMPK profile, and rat oral bioavailability compared to ADS102550.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.

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References

Citations

Hydroxamic acid – A novel molecule for anticancer therapy

Hydroxamic acid derivatives show potential as potent and less toxic anticancer agents by targeting various etiological factors associated with cancer.

Histone deacetylase inhibitors (HDACIs). Structure—activity relationships: history and new QSAR perspectives

Lipophilicity and steric factors are key determinants of anticancer activity in HDAC inhibitors, aiding in the design of new compounds with enhanced inhibitory potencies.

QSAR studies of histone deacetylase (HDAC) inhibitors by CoMFA, CoMSIA, and molecular docking.

3-D QSAR studies using thienyl-based hydroxamic acids can help design highly potent antitumor agents by predicting their activity values and binding modes.

Histone deacetylase inhibitors

HDAC inhibitors show promise in treating cancer and other diseases, with vorinostat being the first approved therapy for advanced cutaneous T cell lymphoma.

A gold(III) porphyrin complex with antitumor properties targets the Wnt/beta-catenin pathway.

Gold-2a shows potential as an antitumor agent by targeting tumor cells with aberrant Wnt/beta-catenin signaling, potentially offering a promising new treatment option for breast cancer.