New 3-aryl-2-(2-thienyl)acrylonitriles with high activity against hepatoma cells was written by Schaller, Eva;Ma, Andi;Gosch, Lisa Chiara;Klefenz, Adrian;Schaller, David;Goehringer, Nils;Kaps, Leonard;Schuppan, Detlef;Volkamer, Andrea;Schobert, Rainer;Biersack, Bernhard;Nitzsche, Bianca;Hoepfner, Michael. And the article was included in International Journal of Molecular Sciences in 2021.Quality Control of 4-(4-Methylpiperazin-1-yl)benzaldehyde This article mentions the following:
New 2-(thien-2-yl)-acrylonitriles with putative kinase inhibitory activity were prepared and tested for their antineoplastic efficacy in hepatoma models. Four out of the 14 derivatives were shown to inhibit hepatoma cell proliferation at (sub-)micromolar concentrations with IC50 values below that of the clin. relevant multikinase inhibitor sorafenib, which served as a reference Colony formation assays as well as primary in vivo examinations of hepatoma tumors grown on the chorioallantoic membrane of fertilized chicken eggs (CAM assay) confirmed the excellent antineoplastic efficacy of the new derivatives Their mode of action included an induction of apoptotic capsase-3 activity, while no contribution of unspecific cytotoxic effects was observed in LDH-release measurements. Kinase profiling of cancer relevant protein kinases identified the two 3-aryl-2-(thien-2-yl)acrylonitrile derivatives 1b and 1c as (multi-)kinase inhibitors with a preferential activity against the VEGFR-2 tyrosine kinase. Addnl. bioinformatic anal. of the VEGFR-2 binding modes by docking and mol. dynamics calculations supported the exptl. findings and indicated that the hydroxy group of 1c might be crucial for its distinct inhibitory potency against VEGFR-2. Forthcoming studies will further unveil the underlying mode of action of the promising new derivatives as well as their suitability as an urgently needed novel approach in HCC treatment. In the experiment, the researchers used many compounds, for example, 4-(4-Methylpiperazin-1-yl)benzaldehyde (cas: 27913-99-1Quality Control of 4-(4-Methylpiperazin-1-yl)benzaldehyde).
4-(4-Methylpiperazin-1-yl)benzaldehyde (cas: 27913-99-1) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Quality Control of 4-(4-Methylpiperazin-1-yl)benzaldehyde
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics