6631-28-3Relevant academic research and scientific papers
Discovery of benzoylsulfonohydrazides as potent inhibitors of the histone acetyltransferase KAT6A
Leaver, David J.,Cleary, Benjamin,Nguyen, Nghi,Priebbenow, Daniel L.,Lagiakos, H. Rachel,Sanchez, Julie,Xue, Lian,Huang, Fei,Sun, Yuxin,Mujumdar, Prashant,Mudududdla, Ramesh,Varghese, Swapna,Teguh, Silvia,Charman, Susan A.,White, Karen L.,Katneni, Kasiram,Cuellar, Matthew,Strasser, Jessica M.,Dahlin, Jayme L.,Walters, Michael A.,Street, Ian P.,Monahan, Brendon J.,Jarman, Kate E.,Sabroux, Helene Jousset,Falk, Hendrik,Chung, Matthew C.,Hermans, Stefan J.,Parker, Michael W.,Thomas, Tim,Baell, Jonathan B.
, p. 7146 - 7159 (2019/08/28)
A high-throughput screen for inhibitors of the histone acetyltransferase, KAT6A, led to identification of an aryl sulfonohydrazide derivative (CTX-0124143) that inhibited KAT6A with an IC50 of 1.0 μM. Elaboration of the structure-activity relationship and medicinal chemistry optimization led to the discovery of WM-8014 (97), a highly potent inhibitor of KAT6A (IC50 = 0.008 μM). WM-8014 competes with acetyl-CoA (Ac-CoA), and X-ray crystallographic analysis demonstrated binding to the Ac-CoA binding site. Through inhibition of KAT6A activity, WM-8014 induces cellular senescence and represents a unique pharmacological tool.
COMPOUNDS CONTAINING A SULFONIC GROUP AS KAT INHIBITORS
-
Paragraph 0382; 0383; 0384; 0385; 0386; 0387, (2018/06/21)
The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
One facile preparation of N-aroyl-N′-arylsulfonylhydrazines by oxidation of aromatic aldehyde N-arylsulfonylhydrazones with bis(trifluoroacetoxy)iodobenzene
Shang, Zhenhua,Reiner, John,Zhao, Kang
, p. 1529 - 1535 (2007/10/03)
N-aroyl-N′-arylsulfonylhydrazines can be obtained by oxidation of aromatic aldehyde N-arylsulfonylhydrazones with bis(trifluoroacetoxy)iodobenzene in acetone at room temperature in mild to good yields. Copyright Taylor & Francis Group, LLC.
