134541-91-6Relevant academic research and scientific papers
NOVEL OXABOROLE ANALOGS AND USES THEREOF
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, (2018/09/21)
This application describes compounds, compositions, and methods which are useful in treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a parasite.
Discovery of a novel 6,7-disubstituted-4-(2-fluorophenoxy)quinolines bearing 1,2,3-triazole-4-carboxamide moiety as potent c-Met kinase inhibitors
Liu, Mingmei,Hou, Yunlei,Yin, Weile,Zhou, Shunguang,Qian, Ping,Guo, Zhuang,Xu, Liying,Zhao, Yangfang
, p. 96 - 108 (2016/05/24)
A series of 6,7-disubstituted-4-(2-fluorophenoxy)quinoline derivatives possessing 1,2,3-triazole-4-carboxamide moiety were designed, synthesized and evaluated for their in vitro cytotoxic activities against four typical cancer cell lines (A549, H460, HT-29, and MKN-45). Most compounds showed moderate-to-excellent antiproliferative activity. Compounds 32, 36, 37, 45, 51, and 52 were further examined for their inhibitory activity against c-Met kinase. The promising compound 37, with a c-Met IC50 value of 2.27 nM, was identified as a multitargeted receptor tyrosine kinase inhibitor. The analysis of their structure-activity relationships indicated that compounds with EWGs, especially chloro group, at 2-position on the phenyl ring (moiety B) have potent antitumor activity.
Triazole containing novobiocin and biphenyl amides as Hsp90 C-terminal inhibitors
Zhao, Jinbo,Zhao, Huiping,Hall, Jessica A.,Brown, Douglas,Brandes, Eileen,Bazzill, Joseph,Grogan, Patrick T.,Subramanian, Chitra,Vielhauer, George,Cohen, Mark S.,Blagg, Brian S. J.
, p. 1317 - 1323 (2014/10/15)
Hsp90 C-terminal inhibitors are advantageous for the development of new cancer chemotherapeutics due to their ability to segregate client protein degradation from induction of the prosurvival heat shock response, which is a major detriment associated with
Synthesis of aminoquinolones from triazoles via carboxamido-ketenimine and amidinoketene intermediates
Rao, V.V. Ramana,Wentrup, Curt
, p. 2583 - 2586 (2007/10/03)
1-Aryl-1H-1,2,3-triazole-4-carboxamides 7d-f have been synthesized and converted to 2-dimethylamino-4-quinolones 12d-f by flash vacuum thermolysis (FVT). The reaction takes place via carboxamidoketenimine 9 and amidinoketene intermediates 10. The former are observed by FTIR spectroscopy at 77 K or in Ar matrices at 12 K.
