832096-07-8Relevant academic research and scientific papers
Dichloroacetophenones targeting at pyruvate dehydrogenase kinase 1 with improved selectivity and antiproliferative activity: Synthesis and structure-activity relationships
Zhang, Shao-Lin,Yang, Zheng,Hu, Xiaohui,Tam, Kin Yip
supporting information, p. 3441 - 3445 (2018/09/29)
Dichloroacetophenone is a pyruvate dehydrogenase kinase 1 (PDK1) inhibitor with suboptimal kinase selectivity. Herein, we report the synthesis and biological evaluation of a series of novel dichloroacetophenones. Structure-activity relationship analyses (SARs) enabled us to identify three potent compounds, namely 54, 55, and 64, which inhibited PDK1 function, activated pyruvate dehydrogenase complex, and reduced the proliferation of NCI-H1975 cells. Mitochondrial bioenergetics assay suggested that 54, 55, and 64 enhanced the oxidative phosphorylation in cancer cells, which might contribute to the observed anti-proliferation effects. Collectively, these results suggested that 54, 55, and 64 could be promising compounds for the development of potent PDK1 inhibitors.
Ultrasound-assisted tandem reaction of alkynes and trihaloisocyanuric acids by thiourea as catalyst in water
Zhang, Xingyu,Wu, Yundong,Zhang, Ya,Liu, Huilan,Xie, Ziyu,Fu, Shengmin,Liu, Fang
, p. 4513 - 4518 (2017/07/10)
With water as the sole solvent, a green and efficient method has been developed for the synthesis of various α,α-dihaloketones via ultrasound assisted p-tolylthiourea catalyzed tandem reaction of alkynes with trihaloisocyanuric acids. This synthetic route
A convenient and efficient synthesis of 1-aryl-2,2-dichloroethanones
Terent'ev, Alexander O.,Khodykin, Sergey V.,Troitskii, Nikolay A.,Ogibin, Yuri N.,Nikishin, Gennady I.
, p. 2845 - 2848 (2007/10/03)
1-Arylethanones are readily chlorinated with an aqueous HCl-H 2O2 system using ethanol as a cosolvent. The reaction prceeds rapidly and results in selective conversion of 1-arylethanones into 1-aryl-2,2-dichloroethanones in yields of 48-89%, depending on the nature of the substituent in the aryl group.
