38214-71-0Relevant articles and documents
Proteasome inhibitors with pyrazole scaffolds from structure-based virtual screening
Miller, Zachary,Kim, Keun-Sik,Lee, Do-Min,Kasam, Vinod,Baek, Si Eun,Lee, Kwang Hyun,Zhang, Yan-Yan,Ao, Lin,Carmony, Kimberly,Lee, Na-Ra,Zhou, Shou,Zhao, Qingquan,Jang, Yujin,Jeong, Hyun-Young,Zhan, Chang-Guo,Lee, Wooin,Kim, Dong-Eun,Kim, Kyung Bo
, p. 2036 - 2041 (2015)
We performed a virtual screen of ~340 000 small molecules against the active site of proteasomes followed by in vitro assays and subsequent optimization, yielding a proteasome inhibitor with pyrazole scaffold. The pyrazole-scaffold compound displayed excellent metabolic stability and was highly effective in suppressing solid tumor growth in vivo. Furthermore, the effectiveness of this compound was not negatively impacted by resistance to bortezomib or carfilzomib.
Proteasome inhibitors
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Page/Page column 33; 34, (2016/12/07)
Compounds of formula (I) are useful for inhibiting a proteasome in a cell. Compounds, pharmaceutical compositions and methods of use are provided herein.
Aluminium complexes containing pyrazolyl-phenolate ligands as catalysts for ring opening polymerization of ε-caprolactone
Huang, Tzu-Lun,Chen, Chi-Tien
, p. 15 - 21 (2013/03/29)
A series of pyrazolyl-phenolate ligand precursors has been described. Reactions of five pyrazolyl-phenolate ligand precursors, HOPh MePzMe, HOPhMePztBu, HOPhMePzPh, HOPhMePz
Synthesis and properties of molecular probes for the rescue site on mutant cystic fibrosis transmembrane conductance regulator
Alkhouri, Bashar,Denning, Robert A.,Chiaw, Patrick Kim,Eckford, Paul D.W.,Yu, Wilson,Li, Canhui,Bogojeski, Jovanka J.,Bear, Christine E.,Viirre, Russell D.
experimental part, p. 8693 - 8701 (2012/03/09)
Cystic fibrosis is a genetic disease caused by mutations in the gene for the cystic fibrosis transmembrane conductance regulator (CFTR) protein. In vitro experiments have demonstrated that 4-methyl-2-(5-phenyl-1H-pyrazol-3-yl)phenol (VRT-532, 1) is able t
Synthesis of pyrazole and isoxazole in triethanolamine medium
Agrawal, Nitin N.,Soni
, p. 532 - 534 (2008/09/18)
Reactions of 2′-hydroxy chalcone dibromides 2a-1 with phenyl hydrazine and hydrazine hydrate afford pyrazoles 1a-1 and with hydroxylamine hydrochloride give isoxazoles 5a-f in triethanolamine medium. Similarly reaction of β-diketone 3b-e with phenyl hydra
PIRAZOLE MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS
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Page 101, (2008/06/13)
The present invention relates to pyrazoles of formula (I) which are modulators of ATP-Binding Cassette ("ABC") transporters or fragments thereof, including Cystic Fibrosis Transmembrane Regulator ("CFTR"), compositions thereof, and methods therewith. The
PYRAZOLES AND ISOXAZOLES DERIVED FROM 2-HYDROXYARYL PHENYLETHYNYL KETONES: SYNTHESIS AND SPECTROPHOTOMETRIC EVALUATION OF THEIR POTENTIAL APPLICABILITY AS SUNSCREENS
Garcia, Heremengildo,Iborra, Sara,Miranda, Miguel A.,Morera, Isabel M.,Primo, Jaime
, p. 1745 - 1755 (2007/10/02)
Reaction of the acetylenic ketones (1) with hydrazine or hydroxylamine leads to the pyrazoles (2) or the isoxazoles (3), respectively.Spectrophotometric evaluation of the UV-photoprotecting ability as compared to p-aminobenzoic acid (PABA) shows that the predicted effectiveness of 2 and the 3-phenylisoxazoles (3B) is very close to that of PABA, while that of the 5-phenylisoxazoles (3A) is clearly lower.The pyrazoles (2) are more stable than PABA upon UV-irradiation in cyclohexane solution.
Reactions of 3-Bromoflavanones with Hydrazine Hydrate
Reddy, N. J.,Sharma, T. C.
, p. 715 - 718 (2007/10/02)
3-Bromoflavanones (I) react with hydrazine hydrate in ethanol to produce pyrazoles (V).The same reaction mixture after 48 hr at room temperature affords pyrazoles (V) and flavones (IV).In acetic acid medium, at room temperature, the reaction products are 3-bromoflavanone hydrazones (III) and flavone azines (II).However, when the reaction mixture is heated, only flavone azines (II) are formed.
Synthesis and Antimicrobial Activity of Hydroxyarylpyrazoles
Sharma, T. C.,Bokadia, M. M.,Reddy, N. J.
, p. 228 - 229 (2007/10/02)
Hydroxyarylpyrazolines (III) and Pyrazoles (IV) have been synthesized.Compounds IVa and IVd exhibit marked antifungal activity against A. niger, C. albicans, C. neoformans, T. mentagraphytes and M. canis whereas compound IVc shows activity against the last three fungi.None of the compounds shows any noteworthy antibacterial activity against Staphy. aureus, Staphi. typhi and Esch. coli even at 100 μg/ml.