13222-37-2Relevant academic research and scientific papers
Reaction of ammonium ylides with alkyl thiocyanates in aqueous and non-aqueous media
Kianmehr, Ebrahim,Mirza Agha, Mansoureh,Estiri, Hamid
, p. 409 - 411 (2010)
Reaction of ammonium ylides with alkyl thiocyanates in aqueous and non-aqueous media is described. The reaction leads to alkyl thio-substituted acetophenones via addition of ammonium ylides to alkyl thiocyanates in organic solvents or in situ generated thiolate anions in aqueous media.
One-pot preparation of arylethynyl sulfides and bis(arylethynyl) sulfides
Su, Qiong,Zhao, Zi-Jian,Xu, Feng,Lou, Peng-Cai,Zhang, Kai,Xie, De-Xun,Shi, Lei,Cai, Qing-Yun,Peng, Zhi-Hong,An, De-Lie
, p. 1551 - 1557 (2013/04/23)
An efficient preparation for arylethynyl sulfides 1 and bis(arylethynyl) sulfides 2 has been accomplished through a one-pot, three-step strategy that starts from arylethanonyl sulfides and bis(arylethanonyl) sulfides, respectively, without the use of various terminal arylacetylenes as substrates. When lithium hexamethyldisilazane (LHMDS), ClP(O)(OEt)2, and LHMDS were sequentially added to a tetrahydrofuran solution of different substrates [arylethanonyl sulfides or bis(arylethanonyl) sulfides], 1 or 2 were obtained in moderate to good yields. The reaction procedure involves the formation of an enol phosphate and a subsequent base-induced elimination. An efficient preparation of arylethynyl sulfides 1 and bis(arylethynyl) sulfides 2 has been accomplished by a one-pot, three-step strategy that starts from arylethanonyl sulfides and bis(arylethanonyl) sulfides, respectively, to give 1 and 2 in moderate to good yields. The reaction mechanism involves the formation of an enol phosphate that undergoes a subsequent base-induced elimination. Copyright
Switching reversibility to irreversibility in glycogen synthase kinase 3 inhibitors: Clues for specific design of new compounds
Perez, Daniel I.,Palomo, Valle,Pérez, Concepción,Gil, Carmen,Dans, Pablo D.,Luque, F. Javier,Conde, Santiago,Martínez, Ana
experimental part, p. 4042 - 4056 (2011/08/05)
Development of kinase-targeted therapies for central nervous system (CNS) diseases is a great challenge. Glycogen synthase kinase 3 (GSK-3) offers a great potential for severe CNS unmet diseases, being one of the inhibitors on clinical trials for different tauopathies. Following our hypothesis based on the enhanced reactivity of residue Cys199 in the binding site of GSK-3, we examine here the suitability of phenylhalomethylketones as irreversible inhibitors. Our data confirm that the halomethylketone unit is essential for the inhibitory activity. Moreover, addition of the halomethylketone moiety to reversible inhibitors turned them into irreversible inhibitors with IC50 values in the nanomolar range. Overall, the results point out that these compounds might be useful pharmacological tools to explore physiological and pathological processes related to signaling pathways regulated by GSK-3 opening new avenues for the discovery of novel GSK-3 inhibitors.
Q39, a novel synthetic Quinoxaline 1,4-Di-N-oxide compound with anti-cancer activity in hypoxia
Weng, Qinjie,Wang, Duoduo,Guo, Peng,Fang, Liang,Hu, Yongzhou,He, Qiaojun,Yang, Bo
, p. 262 - 269 (2008/09/17)
Hypoxia is one of the inevitable circumstances in various tumors and results in tumor resistance to radiotherapy and chemotherapy. The present data showed that 3-(4-bromophenyl)-2-(ethylsulfonyl)-6-methylquinoxaline 1,4-dioxide (Q39), derived from Quinoxa
