Articles with "hydrazide based" as a keyword



Design, synthesis, and biological evaluation of novel amide and hydrazide based thioether analogs targeting Histone deacteylase (HDAC) enzymes.

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Published in 2018 at "European journal of medicinal chemistry"

DOI: 10.1016/j.ejmech.2018.02.011

Abstract: Development of HDAC inhibitors have become an ultimate need targeting different types of cancer. In silico virtual screening was applied to screen novel scaffolds via scaffold hopping strategy to develop different acrylamide and aryl/heteroaryl hydrazide… read more here.

Keywords: hydrazide based; cell lines; based analogs; hdac ... See more keywords

First-in-Class Hydrazide-Based HDAC6 Selective Inhibitor with Potent Oral Anti-Inflammatory Activity by Attenuating NLRP3 Inflammasome Activation.

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Published in 2022 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.2c00853

Abstract: In this study, we report the first highly selective HDAC6 inhibitor with hydrazide as the zinc-binding group (ZBG), which displays superior pharmacokinetic properties to the current hydroxamic acid inhibitors. Structure-activity relationship study reveals that ethyl… read more here.

Keywords: based hdac6; hydrazide; inhibitor; activity ... See more keywords

Exploration of Hydrazide-Based HDAC8 PROTACs for the Treatment of Hematological Malignancies and Solid Tumors

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Published in 2024 at "Journal of Medicinal Chemistry"

DOI: 10.1021/acs.jmedchem.4c00836

Abstract: HDAC8 can mediate signals by using its enzymatic or nonenzymatic functions, which are expected to be critical for various types of cancer. Herein, we employed proteolysis targeting chimera (PROTAC) technology to target the enzymatic as… read more here.

Keywords: protacs treatment; exploration hydrazide; based hdac8; hydrazide based ... See more keywords

Development of Hydrazide-Based HDAC6 Selective Inhibitors for Treating NLRP3 Inflammasome-Related Diseases.

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Published in 2025 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.4c02883

Abstract: Previously, we found that hydrazide can serve as zinc binding groups for selective HDAC6 inhibitors and identified the first hydrazide-based HDAC6 inhibitor, 35m, which exhibited modest isoform selectivity. This study aimed to improve the HDAC6… read more here.

Keywords: nlrp3 inflammasome; hydrazide based; related diseases; inflammasome related ... See more keywords