111016-46-7Relevant articles and documents
4-Aryl-1,2,3-triazole: A novel template for a reversible methionine aminopeptidase 2 inhibitor, optimized to inhibit angiogenesis in vivo
Kallander, Lara S.,Lu, Qing,Chen, Wenfang,Tomaszek, Thaddeus,Yang, Guang,Tew, David,Meek, Thomas D.,Hofmann, Glenn A.,Schulz-Pritchard, Christina K.,Smith, Ward W.,Janson, Cheryl A.,Ryan, M. Dominic,Zhang, Gui-Feng,Johanson, Kyung O.,Kirkpatrick, Robert B.,Ho, Thau F.,Fisher, Paul W.,Mattern, Michael R.,Johnson, Randall K.,Hansbury, Michael J.,Winkler, James D.,Ward, Keith W.,Veber, Daniel F.,Thompson, Scott K.
, p. 5644 - 5647 (2005)
Inhibitors of human methionine aminopeptidase type 2 (hMetAP2) are of interest as potential treatments for cancer. A new class of small molecule reversible inhibitors of hMetAP2 was discovered and optimized, the 4-aryl-1,2,3-triazoles. Compound 24, a potent inhibitor of cobalt-activated hMetAP2, also inhibits human and mouse endothelial cell growth. Using a mouse matrigel model, this reversible hMetAP2 inhibitor was also shown to inhibit angiogenesis in vivo.
Synthesis and biological evaluation of some novel N-arylpyrazole derivatives as cytotoxic agents
Li, Shenghui,Xu, Shengjie,Ding, Shan,Zhang, Jinchao,Wang, Shuxiang,Li, Xiaoliu
, p. 1459 - 1468 (2014/05/06)
A series of novel N-arylpyrazole derivatives, 5a-5i, were achieved from substituted phenylacetic acid via Vilsmeier-Haack reaction, hydrolysis, condensation, and aromatic substitution reaction. Their chemical structures were confirmed by 1H NMR
Synthesis and reactions of some ethyl 3(5)aroyl-4-aryl-2-pyrazoline-5(3)carboxylates
Faidallah, Hassan M.,Makki, Mohamed S. I.,El-Massry, Abdel-Moneium I.,Hassan, Saham Y.
, p. 1141 - 1153 (2007/10/03)
A series of ethyl 3(5)aroyl-4-aiyl-2-pyrazoline-5(3)carboxylates 1 was prepared. Their reactions with bromine water, potassium permanganate and potassium hydroxide afforded the corresponding pyrazoles. With aryl and aroyl hydrazines the pyrazolines 1 gave the Schiff bases 9 while with hydrazine hydrate they yielded the corresponding acid hydrazides 11. Condensation of 11 with aromatic aldehydes gave the arylidene derivatives 12, which, on cyclization with the propar reagent, afforded 13 or 14. Reaction of 1 with hydrochloric acid gave the corresponding dipyrazolo-pyrazine derivatives 10.
