781663-68-1Relevant academic research and scientific papers
Discovery and evaluation of Cav3.1-selective T-type calcium channel blockers
Bezen?on, Olivier,Remeň, Lubo?,Richard, Sylvia,Roch, Catherine,Kessler, Melanie,Moon, Richard,Mawet, Jacques,Ertel, Eric A.,Pfeifer, Thomas,Capeleto, Bruno
, p. 5322 - 5325 (2017/10/26)
We identified and characterized a series of pyrazole amides as potent, selective Cav3.1-blockers. This series culminated with the identification of pyrazole amides 5a and 12d, with excellent potencies and/or selectivities toward the Cav3.2- and Cav3.3-channels. This compound displays poor DMPK properties, making its use difficult for in vivo applications. Nevertheless, this compound as well as analogous ones are well-suited for in vitro studies.
A new efficient synthesis of pyrazoles from hydrazonoyl halides and β-oxophosphonates
Sun, Aixue,Ye, Jia-Hai,Yu, Haitao,Zhang, Wenchao,Wang, Xiaolong
supporting information, p. 889 - 892 (2015/03/03)
A new practical and efficient synthesis of 1,3,5-trisubstituted pyrazoles has been developed by reacting of hydrazonoyl halides with β-oxophosphonates under mild conditions in good yields with excellent regioselectivity. This process employs an addition-elimination sequence. Wide scope, functional group compatibility has been established.
A new efficient synthesis of pyrazoles from hydrazonoyl halides and β-oxophosphonates
Sun, Aixue,Ye, Jia-Hai,Yu, Haitao,Zhang, Wenchao,Wang, Xiaolong
supporting information, p. 889 - 892 (2014/02/14)
A new practical and efficient synthesis of 1,3,5-trisubstituted pyrazoles has been developed by reacting of hydrazonoyl halides with β- oxophosphonates under mild conditions in good yields with excellent regioselectivity. This process employs an addition-elimination sequence. Wide scope, functional group compatibility has been established.
New COX-2/5-LOX inhibitors: Apoptosis-inducing agents potentially useful in prostate cancer chemotherapy
Pommery, Nicole,Taverne, Thierry,Telliez, Aurélie,Goossens, Laurence,Charlier, Caroline,Pommery, Jean,Goossens, Jean-Fran?ois,Houssin, Raymond,Durant, Fran?ois,Hénichart, Jean-Pierre
, p. 6195 - 6206 (2007/10/03)
The arachidonic acid metabolizing enzymes cyclooxygenase-2 (COX-2) and lipoxygenases (LOXs) have been found to be implicated in a variety of cancers, including prostate cancer. To develop new therapeutic treatments, it therefore seemed interesting to design dual COX-2/5-LOX inhibitors. We report here the synthesis and in vitro pharmacological properties of diarylpyrazole derivatives that have in their structure key pharmacophoric elements to obtain optimal interaction with subsites of active pockets in both enzyme systems. Using a molecular modeling approach, a set of SAR data is proposed, highlighting the importance of the sulfonyl group of one of the aryl moieties in terms of proliferation inhibition and/or apoptosis induction.
