69321-56-8Relevant articles and documents
A scaffold replacement approach towards new sirtuin 2 inhibitors
Seifert, Tina,Malo, Marcus,Kokkola, Tarja,Stéen, E. Johanna L.,Meinander, Kristian,Wallén, Erik A.A.,Jarho, Elina M.,Luthman, Kristina
, (2019/12/24)
Sirtuins (SIRT1–SIRT7) are an evolutionary conserved family of NAD+-dependent protein deacylases regulating the acylation state of ε-N-lysine residues of proteins thereby controlling key biological processes. Numerous studies have found association of the aberrant enzymatic activity of SIRTs with various diseases like diabetes, cancer and neurodegenerative disorders. Previously, we have shown that substituted 2-alkyl-chroman-4-one/chromone derivatives can serve as selective inhibitors of SIRT2 possessing an antiproliferative effect in two human cancer cell lines. In this study, we have explored the bioisosteric replacement of the chroman-4-one/chromone core structure with different less lipophilic bicyclic scaffolds to overcome problems associated to poor physiochemical properties due to a highly lipophilic substitution pattern required for achieve a good inhibitory effect. Various new derivatives based on the quinolin-4(1H)-one scaffold, bicyclic secondary sulfonamides or saccharins were synthesized and evaluated for their SIRT inhibitory effect. Among the evaluated scaffolds, the benzothiadiazine-1,1-dioxide-based compounds showed the highest SIRT2 inhibitory activity. Molecular modeling studies gave insight into the binding mode of the new scaffold-replacement analogues.
Aryl sulfide derivatives and aryl sulfoxide derivatives as acaricides and insecticides
-
Paragraph 1874; 1875; 1876; 187, (2016/10/08)
The invention relates to aryl sulfide derivatives and aryl sulfoxide derivatives, use thereof as acaricides and insecticides for controlling animal pests, and methods and intermediate products for the production thereof. The aryl sulfide derivatives and a
Optimization of heterocyclic substituted benzenesulfonamides as novel carbonic anhydrase IX inhibitors and their structure activity relationship
Gao, Rui,Liao, Sha,Zhang, Chen,Zhu, Weilong,Wang, Liyan,Huang, Jin,Zhao, Zhenjiang,Li, Honglin,Qian, Xuhong,Xu, Yufang
, p. 597 - 604 (2013/05/09)
In this study, starting from a lead compound discovered by virtual screening, a series of novel heterocyclic substituted benzenesulfonamides were designed and synthesized as new carbonic anhydrase IX (CA IX) inhibitors. Some compounds exhibited potent inh