1578-89-8Relevant articles and documents
Design, synthesis and anticancer activity of some novel 5-(4-methoxyphenyl)-2,4-dihydro-3H-pyrazol-3-one derivatives
Fathy, Usama,Gouhar, Rasha S.,Awad, Hanem M.
, p. 1427 - 1436 (2017/10/23)
New pyrazole derivatives were designed and synthesized by the reaction of 5-(4-methoxyphenyl)-2,4-dihydro-3H-pyrazol-3-one (4) or 5-(4-methoxyphenyl)-2-phenyl-2,4-dihydro-3H-pyrazol-3-one (5) with series of aldehydes, substituted amines, isatins and phenylisothiocynate to yield 6a-j, 7a-k, 9a-d and 10a-b, respectively. The synthesized compounds were examined in vitro for their anti-tumor activities against HepG-2, PC-3 and HCT-116 human carcinoma cell lines using MTT assay. Eight compounds showed good anticancer activities against HCT-116 carcinoma cells and five compounds showed good anticancer activities against PC-3 cancer cells but all the compounds showed weak or no anticancer activities against HepG-2 liver cancer.
3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3β
Arnost, Michael,Pierce, Al,Haar, Ernst ter,Lauffer, David,Madden, Jaren,Tanner, Kirk,Green, Jeremy
scheme or table, p. 1661 - 1664 (2010/07/03)
A series of 3-aryl-4-(arylhydrazono)-1H-pyrazol-5-one inhibitors of GSK3β was developed from a low molecular weight, highly ligand efficient screening hit 1. Hit-to-lead optimization led to a number of highly potent inhibitors, while maintaining the high ligand efficiency of the screening hit.