Results 171 to 180 of about 8,600 (184)

Design and synthesis of non-hydroxamate histone deacetylase inhibitors: identification of a selective histone acetylating agent

Bioorganic & Medicinal Chemistry, 2005
A series of suberoylanilide hydroxamic acid (SAHA)-based non-hydroxamates was designed, synthesized, and evaluated for their histone deacetylase (HDAC) inhibitory activity. Among these, methyl sulfoxide 15 inhibited HDACs in enzyme assays and caused hyperacetylation of histone H4 while not inducing the accumulation of acetylated alpha-tubulin in HCT116
Takayoshi, Suzuki, Azusa, Matsuura, Akiyasu, Kouketsu, Shinya, Hisakawa, Hidehiko, Nakagawa, Naoki, Miyata   +5 more
openaire   +2 more sources

Hydantoins, triazolones, and imidazolones as selective non-hydroxamate inhibitors of tumor necrosis factor-α converting enzyme (TACE)

Bioorganic & Medicinal Chemistry Letters, 2007
We have discovered selective and potent inhibitors of TACE that replace the common hydroxamate zinc binding group with a hydantoin, triazolone, and imidazolone heterocycle. These novel heterocyclic inhibitors of a zinc metalloprotease were designed using a pharmacophore model that we previously described while developing hydantoin and pyrimidinetrione (
James E, Sheppeck, John L, Gilmore, Andrew, Tebben, Chu-Biao, Xue, Rui-Qin, Liu, Carl P, Decicco, James J-W, Duan   +6 more
openaire   +2 more sources

Synthesis and activity of tryptophan sulfonamide derivatives as novel non-hydroxamate TNF-α converting enzyme (TACE) inhibitors

Bioorganic & Medicinal Chemistry, 2009
A novel series of non-hydroxamate tryptophan sulfonamide derivatives containing a butynyloxy P1' moiety was identified as inhibitors of TNF-alpha converting enzyme (TACE). The structure-activity relationship of the series was examined via substitution on the tryptophan indole ring. Of the compounds investigated, 2-(4-(but-2-ynyloxy)phenylsulfonamido)-3-
Kaapjoo, Park, Ariamala, Gopalsamy, Alexis, Aplasca, John W, Ellingboe, Weixin, Xu, Yuhua, Zhang, Jeremy I, Levin   +6 more
openaire   +2 more sources

Non-hydroxamate 5-phenylpyrimidine-2,4,6-trione derivatives as selective inhibitors of tumor necrosis factor-α converting enzyme

Bioorganic & Medicinal Chemistry Letters, 2005
New inhibitors of tumor necrosis factor-alpha converting enzyme (TACE) were discovered with a pyrimidine-2,4,6-trione in place of the commonly used hydroxamic acid. These non-hydroxamate TACE inhibitors were developed by incorporating a 4-(2-methyl-4-quinolinylmethoxy)phenyl group, an optimized TACE selective P1' group.
James J-W, Duan, Zhonghui, Lu, Zelda R, Wasserman, Rui-Qin, Liu, Maryanne B, Covington, Carl P, Decicco   +5 more
openaire   +2 more sources

Synthesis and structure–activity relationship of a novel, non-hydroxamate series of TNF-α converting enzyme inhibitors

Bioorganic & Medicinal Chemistry Letters, 2007
A novel series of TNF-alpha converting enzyme (TACE) inhibitors which are non-hydroxamate have been discovered. These compounds use a triazolethione moiety as the zinc binding ligand and exhibit IC50 values from 1.5 to 100 nM in a porcine TACE assay. They also have excellent selectivities over other MMPs.
John L, Gilmore, Bryan W, King, Naoyuki, Asakawa, Kimberly, Harrison, Andrew, Tebben, James E, Sheppeck, Rui-Qin, Liu, Maryanne, Covington, James J-W, Duan   +8 more
openaire   +2 more sources

Medicinal chemistry insights into non-hydroxamate HDAC6 selective inhibitors

Medicinal Chemistry Research, 2022
null Faridoon, Yuqi Lavender Zha, Guiping Zhang, Jie Jack Li   +3 more
openaire   +1 more source

Investigation of non-hydroxamate scaffolds against HDAC6 inhibition: A pharmacophore modeling, molecular docking, and molecular dynamics simulation approach

Journal of Bioinformatics and Computational Biology, 2018
Proteins deacetylation by Histone deacetylase 6 (HDAC6) has been shown in various human chronic diseases like neurodegenerative diseases and cancer, and hence is an important therapeutic target. Since, the existing inhibitors have hydroxamate group, and are not HDAC6-selective, therefore, this study has designed to investigate non-hydroxamate HDAC6 ...
Amir, Zeb, Chanin, Park, Minky, Son, Shailima, Rampogu, Syed Ibrar, Alam, Seok Ju, Park, Keun Woo, Lee   +6 more
openaire   +2 more sources

A semiempirical and machine learning approach for fragment-based structural analysis of non-hydroxamate HDAC3 inhibitors

Biophysical Chemistry
Interest in HDAC3 inhibitors (HDAC3i) for pharmacological applications outside of cancer is growing. However, concerns regarding the possible mutagenicity of the commonly used hydroxamates (zinc-binding groups, ZBGs) are also increasing. Considering these concerns, non-hydroxamate ZBGs offer a promising alternative for the development of non-mutagenic ...
Amin, Sk. Abdul, Sessa, Lucia, Tarafdar, Rajdip, Gayen, Shovanlal, Piotto, Stefano   +4 more
openaire   +2 more sources

Evaluation of Zinc Chelation Ability for Non-Hydroxamic Organic Moieties

Egyptian Journal of Chemistry, 2022
Ayad Al-Hamashi, Shayma Abdulhadi, Rusul Ali   +2 more
openaire   +1 more source

Design and synthesis of novel Hydroxamate and non-Hydroxamate HDAC inhibitors based on Chromone and Quinazolone scaffolds

Bioorganic Chemistry
The development of selective histone deacetylase (HDAC) inhibitors represents an encouraging approach for cancer therapy. In this study, we report design, synthesis, and biological evaluation of hydroxamate, amidoxime, and carboxylic acid-based derivatives as novel HDAC inhibitors.
Rosaline, Ashraf, Mai, Adel, Rabah A T, Serya, Esraa, Ibrahim, Hesham, Haffez, Sameh, Soror, Khaled A M, Abouzid   +6 more
openaire   +2 more sources