98534-76-0Relevant academic research and scientific papers
Pyrazole-4-Carboxamide (YW2065): A Therapeutic Candidate for Colorectal Cancer via Dual Activities of Wnt/β-Catenin Signaling Inhibition and AMP-Activated Protein Kinase (AMPK) Activation
Yang, Wei,Li, Yingjun,Ai, Yong,Obianom, Obinna N.,Guo, Dong,Yang, Hong,Sakamuru, Srilatha,Xia, Menghang,Shu, Yan,Xue, Fengtian
, p. 11151 - 11164 (2019/12/27)
Dysregulation of the Wnt/β-catenin signaling pathway has been widely recognized as a pathogenic mechanism for colorectal cancer (CRC). Although numerous Wnt inhibitors have been developed, they commonly suffer from toxicity and unintended effects. Moreover, concerns have been raised in targeting this pathway because of its critical roles in maintaining stem cells and regenerating tissues and organs. On the basis of the anthelmintic drug pyrvinium and previous lead FX1128, we have developed a compound YW2065 (1c) which demonstrated excellent anti-CRC effects in vitro and in vivo. YW2065 achieves its inhibitory activity for Wnt signaling by stabilizing Axin-1, a scaffolding protein that regulates proteasome degradation of β-catenin. Simultaneously, YW2065 also led to the activation of the tumor suppressor AMPK, providing an additional anticancer mechanism. In addition, YW2065 showed favorable pharmacokinetic properties without obvious toxicity. The anti-CRC effect of YW2065 was highlighted by its promising efficacy in a mice xenograft model.
Heterocyclic analogues of xanthone and xanthione. 1H-pyrano[2,3-c:6,5-c] dipyrazol-4(7H)-ones and thiones: Synthesis and NMR data
Datterl, Barbara,Troestner, Nicole,Kucharski, Dorota,Holzer, Wolfgang
experimental part, p. 6106 - 6126 (2010/11/04)
The synthesis of the title compounds is described. Reaction of 1-substituted 2-pyrazolin-5-ones with 5-chloro-1-phenyl-1H-pyrazole-4-carbonyl chloride or 5-chloro-3-methyl-1-phenyl-1H-pyrazole-4-carbonyl chloride, respectively, using calcium hydroxide in refluxing 1,4-dioxane gave the corresponding 4-heteroaroylpyrazol-5-ols, which were cyclized into 1H-pyrano[2,3-c:6,5-c]dipyrazol-4(7H)-ones by treatment with K 2CO3/DMF. The latter were converted into the corresponding thiones upon reaction with Lawesson's reagent. Detailed NMR spectroscopic investigations (1H, 13C, 15N) of the ring systems and their precursors are presented.
Inhibitors of 11B-Hyrdoxysteroid Dehydrogenase
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Page/Page column 11, (2009/02/11)
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful
Nonaqueous Diazotation of 5-Amino-1-aryl-1H-pyrazole-4-carboxylate Esters
Beck, James R.,Gajewski, Robert P.,Lynch, Michael P.,Wright, Fred L.
, p. 267 - 270 (2007/10/02)
5-Amino-1-aryl-1H-pyrazole-4-carboxylate esters are converted to the corresponding desamino, chloro, bromo, iodo, and methylthio esters by processes involving nonaqueous diazotation.Diazotizing agents are alkyl nitrites except in the case of chlorine wher
