1578-89-8Relevant academic research and scientific papers
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.
POLYCYCLIC DERIVATIVES TARGETING RAL GTPASES AND THEIR THERAPEUTICAL APPLICATIONS
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Paragraph 0158-0159, (2017/01/02)
Contemplated compounds, compositions and methods are directed to Ral GTPase inhibitors with improved activity.
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.
QUINAZOLINE DERIVATIVES
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Page/Page column 32, (2010/02/11)
The invention relates to the use of compounds of the formula I: wherein: ring C is a 5-6 membered heterocyclic moiety; Z is -O-, -S-, or -CH2-; R1 is hydrogen, C1-4alkyl, C1-4alkoxymethyl, di(C1-4)alkoxy)methyl, C1-4alkanoyl, trifluoromethyl, cyano, amino, C2-5alkenyl, C2-5alkynyl, carboxy, C3-7cycloalkyl, C3-7-cycloalkylC1-3alkyl, or an optionally substituted group selected from phenyl, benzyl, phenylC2-4alkyl and a 5-6 membered heterocyclic group; n is an integer from 0 to 5; m is an integer from 0 to 3; R2 represents hydrogen, hydroxy, halgeno, cyano, nitro, trifluoromethyl, C1-3alkyl, C1-3alkoxy, C1-3alkylsulphanyl, -NR3R4 (wherein R3 and R4, which may be the same or different, each represents hydrogen or C1-3alkyl), or R5X1- (wherein X1 represents a direct bond, -CH2-, or a heteroatom linker group and R5 is an alkyl, alkenyl or alkynyl chain optionally substituted by for example hydroxy, amino, nitro, alkyl, cycloalkyl, alkoxyalkyl, or an optionally substituted group selected from pyridone, phenyl and a heterocyclic ring, which alkyl, alkenyl or alkynyl chain may have a heteroatom linker group, or R5 is an optionally substituted group selected from pyridone, phenyl and a heterocyclic ring, and salts thereof, in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals, processes for the preparation of such compounds, pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof as active ingredient and compounds of formula I. The compounds of formula I and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.
