14058-84-5Relevant academic research and scientific papers
Design and biological evaluation of novel 4-(2-fluorophenoxy)quinoline derivatives bearing an imidazolone moiety as c-Met kinase inhibitors
Liao, Weike,Hu, Gang,Guo, Zhuang,Sun, Deyu,Zhang, Lixia,Bu, Yanxin,Li, Yingxiu,Liu, Yajing,Gong, Ping
, p. 4410 - 4422 (2015/08/03)
A series of 4-(2-fluorophenoxy)quinoline derivatives containing an imidazolone moiety were designed, synthesized and evaluated for their in vitro biological activities against c-Met kinase and four cancer cell lines (A549, H460, HT-29 and MKN-45). Most compounds showed moderate to excellent activities in enzyme and cellular assays. The most promising analog, 58 (c-Met IC50 = 1.42 nM), displayed 2.1-, 8.6-fold increase against H460, and MKN-45 cell lines, respectively, compared with foretinib. An analysis of structure-activity relationships revealed that an ortho substituted phenyl ring as well as an N-unsubstituted imidazolone linker is favorable for antitumor activity.
N-H insertion reactions of primary ureas: The synthesis of highly substituted imidazolones and imidazoles from diazocarbonyls
Lee, Sang-Hyeup,Yoshida, Kazuhiro,Matsushita, Hana,Clapham, Bruce,Koch, Guido,Zimmermann, Juerg,Janda, Kim D.
, p. 8829 - 8835 (2007/10/03)
Primary ureas have been used as substrates in rhodium-catalyzed N-H insertion reactions with an array of diazocarbonyls. The insertion reaction is efficient and gives excellent selectivity and yields. The products from the insertion reaction with diazoket
Rhodium carbenoid N-H insertion reactions of primary ureas: solution and solid-phase synthesis of imidazolones.
Lee, Sang-Hyeup,Clapham, Bruce,Koch, Guido,Zimmermann, Juerg,Janda, Kim D
, p. 511 - 514 (2007/10/03)
[reaction: see text] The solution and solid-phase synthesis of imidazolones is reported. The key step for the preparation of these compounds is the N-H insertion reaction of primary ureas into highly reactive rhodium carbenoid intermediates. Typically, a
