Dataset Information

Improved Selective Class I HDAC and Novel Selective HDAC3 Inhibitors: Beyond Hydroxamic Acids and Benzamides.

ABSTRACT: The application of class I HDAC inhibitors as cancer therapies is well established, but more recently their development for nononcological indications has increased. We report here on the generation of improved class I selective human HDAC inhibitors based on an ethylketone zinc binding group (ZBG) in place of the hydroxamic acid that features the majority of HDAC inhibitors. We also describe a novel set of HDAC3 isoform selective inhibitors that show stronger potency and selectivity than the most commonly used HDAC3 selective tool compound RGFP966. These compounds are again based on an alternative ZBG with respect to the ortho-anilide that is featured in HDAC3 selective compounds reported to date.

SUBMITTER: Bresciani A

PROVIDER: S-EPMC6466521 | biostudies-literature | 2019 Apr

REPOSITORIES: biostudies-literature

ACCESS DATA

Publications

Improved Selective Class I HDAC and Novel Selective HDAC3 Inhibitors: Beyond Hydroxamic Acids and Benzamides.

Bresciani Alberto A Ontoria Jesus M JM Biancofiore Ilaria I Cellucci Antonella A Ciammaichella Alina A Di Marco Annalise A Ferrigno Federica F Francone Alessandra A Malancona Savina S Monteagudo Edith E Nizi Emanuela E Pace Paola P Ponzi Simona S Rossetti Ilaria I Veneziano Maria M Summa Vincenzo V Harper Steven S

ACS medicinal chemistry letters 20181127 4

The application of class I HDAC inhibitors as cancer therapies is well established, but more recently their development for nononcological indications has increased. We report here on the generation of improved class I selective human HDAC inhibitors based on an ethylketone zinc binding group (ZBG) in place of the hydroxamic acid that features the majority of HDAC inhibitors. We also describe a novel set of HDAC3 isoform selective inhibitors that show stronger potency and selectivity than the mo ...[more]

PMID: 30996783

Dataset Information

Improved Selective Class I HDAC and Novel Selective HDAC3 Inhibitors: Beyond Hydroxamic Acids and Benzamides.

Publications

Improved Selective Class I HDAC and Novel Selective HDAC3 Inhibitors: Beyond Hydroxamic Acids and Benzamides.

Similar Datasets

OmicsDI is part of the ELIXIR infrastructure

Tweets

Similar Datasets

Hydroxamic Acids Immobilized on Resins (HAIRs): Synthesis of Dual-Targeting HDAC Inhibitors and HDAC Degraders (PROTACs).
| S-EPMC7756583 | biostudies-literature

Discovering HDAC class II selective inhibitors by multidisciplinary approach
| S-EPMC3083574 | biostudies-literature

Synthesis and HDAC inhibitory activity of pyrimidine-based hydroxamic acids.
| S-EPMC9296983 | biostudies-literature

Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
| S-EPMC7238858 | biostudies-literature

Selective class II HDAC inhibitors impair myogenesis by modulating the stability and activity of HDAC-MEF2 complexes.
| S-EPMC2693879 | biostudies-literature

Selective class II HDAC inhibitors impair myogenesis by modulating the stability and activity of HDAC-MEF2 complexes.
| S-EPMC7726812 | biostudies-literature

N-alkyl urea hydroxamic acids as a new class of peptide deformylase inhibitors with antibacterial activity.
| S-EPMC127453 | biostudies-literature

Potent, Selective, and CNS-Penetrant Tetrasubstituted Cyclopropane Class IIa Histone Deacetylase (HDAC) Inhibitors.
| S-EPMC4716601 | biostudies-literature

Oxazole-Bridged Combretastatin A-4 Derivatives with Tethered Hydroxamic Acids: Structure⁻Activity Relations of New Inhibitors of HDAC and/or Tubulin Function.
| S-EPMC6359144 | biostudies-literature

Hydroxamic Acid-Based Histone Deacetylase (HDAC) Inhibitors Bearing a Pyrazole Scaffold and a Cinnamoyl Linker.
| S-EPMC6412695 | biostudies-literature