scholarly journals Aromatic side-chain flips orchestrate the conformational sampling of functional loops in Human Histone Deacetylase 8

2021 ◽  
Author(s):  
Vaibhav Kumar Shukla ◽  
Lucas Siemons ◽  
Francesco Gervasio ◽  
Flemming Hansen
Keyword(s):  
Gene Regulation ◽  
High Resolution ◽  
Histone Deacetylase ◽  
Drug Target ◽  
Side Chain ◽  
Conformational Sampling ◽  
Aromatic Side Chain ◽  
Histone Deacetylase 8 ◽  
Important Drug

Human histone deacetylase 8 (HDAC8) is a key hydrolase in gene regulation and an important drug-target. High-resolution structures of HDAC8 in complex with substrates or inhibitors are available, which have...

ChemInform Abstract: Synthesis of Side Chain Modified Apicidin Derivatives: Potent Mechanism-Based Histone Deacetylase Inhibitors

ChemInform ◽  
2000 ◽  
Vol 31 (52) ◽  
pp. no-no
Author(s):  
Peter T. Meinke ◽  
Steven L. Colletti ◽  
Michelle B. Ayer ◽  
Sandra J. Darkin-Rattray ◽  
Robert W. Myers ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Histone Deacetylase Inhibitors ◽  
Side Chain

Synthesis of Substituted -N-(5-((7-Methyl-2-Oxo-2H-Chromen-4-yl)-Methyl)-1,3,4-Thiadiazol-2-yl)-Benzamide Derivatives Using TBTU As Coupling Agent And Their Evaluation For Anti Tubercular Activity

2021 ◽  
Vol 18 ◽  
Author(s):  
Monika Kakadiya ◽  
Yunus Pasha ◽  
Malleshappa Noolvi ◽  
Ashish Patel
Keyword(s):  
Antitubercular Activity ◽  
Side Chain ◽  
Antitubercular Agents ◽  
Facile Synthesis ◽  
Aromatic Side Chain ◽  
Reaction Conditions ◽  
Coupling Reagent ◽  
H37rv Strain ◽  
Benzamide Derivatives

: Tuberculosis remains a highly infectious disease across the world. In the identification of new antitubercular agents, coumarin clubbed thiadiazole amides have been synthesized and evaluated for in vitro antitubercular activity. Due to the growing concern about chemicals and their impact on the environment, greener and faster reaction conditions needed to be incorporated. Therefore, we used TBTU as a coupling reagent for efficient and facile synthesis of substituted-N-(5-((7-methyl-2-oxo-2H-chromes-4-yl)-methyl)-1,3, 4 - thiadiazol-2-yl)-benzamide 4a-j with good yields up to 95% in mild reaction condition. All the synthesized compounds were evaluated in vitro for antitubercular activity against the H37Rv strain of M.Tuberculosis. Compounds 4c, 4f, and 4j were found active at 25 µg/mL against M. tb H37Rv. Electron withdrawing substituents present on aromatic side-chain showed promising anti-tubercular activity.

Rapid Discovery of Highly Potent and Selective Inhibitors of Histone Deacetylase 8 Using Click Chemistry to Generate Candidate Libraries

2012 ◽  
Vol 55 (22) ◽  
pp. 9562-9575 ◽  
Author(s):  
Takayoshi Suzuki ◽  
Yosuke Ota ◽  
Masaki Ri ◽  
Masashige Bando ◽  
Aogu Gotoh ◽  
...  
Keyword(s):  
Click Chemistry ◽  
Histone Deacetylase ◽  
Selective Inhibitors ◽  
Histone Deacetylase 8

scholarly journals The inhibition of histone deacetylase 8 suppresses proliferation and inhibits apoptosis in gastric adenocarcinoma

2015 ◽  
Vol 47 (5) ◽  
pp. 1819-1828 ◽  
Author(s):  
SHIYUAN SONG ◽  
YING WANG ◽  
PO XU ◽  
RUINA YANG ◽  
ZHIKUN MA ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Gastric Adenocarcinoma ◽  
Histone Deacetylase 8

Histone deacetylase 8 (HDAC8) and its inhibitors with selectivity to other isoforms: An overview

2019 ◽  
Vol 164 ◽  
pp. 214-240 ◽  
Author(s):  
Suvankar Banerjee ◽  
Nilanjan Adhikari ◽  
Sk Abdul Amin ◽  
Tarun Jha
Keyword(s):  
Histone Deacetylase ◽  
Histone Deacetylase 8

scholarly journals Characterization of Histone Deacetylase 8 (HDAC8) Selective Inhibition Reveals Specific Active Site Structural and Functional Determinants

2018 ◽  
Vol 61 (22) ◽  
pp. 10000-10016 ◽  
Author(s):  
Martin Marek ◽  
Tajith B. Shaik ◽  
Tino Heimburg ◽  
Alokta Chakrabarti ◽  
Julien Lancelot ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Active Site ◽  
Selective Inhibition ◽  
Histone Deacetylase 8
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