93019-39-7Relevant 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.
Haloacetylated enol ethers. 11 [16]. Synthesis of 1-methyl- and 1- phenyl pyrazole-3(5)-ethyl esters. A one-pot procedure
Martins, Marcos A. P.,Freitag, Rogerio A.,Da Rosa, Adriano,Flores, Alex F. C.,Zanatta, Nilo,Bonacorso, Helio G.
, p. 217 - 220 (2007/10/03)
A one-pot synthesis of 1-methyl- and 1-phenylpyrazole-3(5)-ethyl esters 2,3a-e by the cyclocondensation of β-alkoxyvinyl trichloromethyl ketones 1a- e with methyl and phenyl hydrazine hydrochloride under mild conditions, is reported. A study using compounds la-e with different substituents proved that these are versatile building blocks for the synthesis of pyrazole derivatives, having a 3(5)-ethoxycarbonyl substituent in good yields (60- 89%). The hydrazine and β-alkoxyvinyl trichloromethyl ketone substituent effects on the reaction regiochemistry on the formation of the 1,3- and 1,5- isomer were observed.
Cyclopentapyrazole and tetrahydroindazole compounds and their use as anti-inflammatory and anti-allergic agents
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, (2008/06/13)
The present invention provides novel compositions of matter and their therapeutic applications. More particularly, the present invention consists of novel cyclopentapyrazole and tetrahydroindazole compounds of formula XXX and their use as antiallergy agents, antiinflammatory agents or intermediates. STR1
