104236-78-4Relevant academic research and scientific papers
Design, synthesis and SAR study of hydroxychalcone inhibitors of human β-secretase (BACE1)
Ma, Lei,Yang, Zhengyi,Li, Chenjing,Zhu, Zhiyuan,Shen, Xu,Hu, Lihong
, p. 643 - 648 (2012/04/10)
According to the structural characteristics of isoliquiritigenin from Glycyrrhiza uralensis, a series of hydroxychalcones has been designed, synthesized and evaluated for their in vitro inhibitory activities of β-secretase (BACE1). Structure-activity relationship study suggested that inhibitory activity against BACE1 was governed to a greater extent by the hydroxyl substituent on A-and B-ring of the chalcone, and the most active compound was substituted with four hydroxyl group (17, IC50=0.27 μM).
Synthesis of some pyrazole derivatives and preliminary investigation of their affinity binding to P-glycoprotein
Manna, Fedele,Chimenti, Franco,Fioravanti, Rossella,Bolasco, Adriana,Secci, Daniela,Chimenti, Paola,Ferlini, Cristiano,Scambia, Giovanni
, p. 4632 - 4635 (2007/10/03)
A series of substituted pyrazolines were synthesized and evaluated for their anticancer activity and for their ability to inhibit P-glycoprotein- mediated multidrug resistance by direct binding to a purified protein domain containing an ATP-binding site and a modulator interacting region. Compounds 2a and e have been found to bind to P-glycoprotein with greater affinity.
Synthesis and Selective Inhibitory Activity of 1-Acetyl-3,5-diphenyl-4,5-dihydro-(1H)-pyrazole Derivatives against Monoamine Oxidase
Chimenti, Franco,Bolasco, Adriana,Manna, Fedele,Secci, Daniela,Chimenti, Paola,Befani, Olivia,Turini, Paola,Giovannini, Valentina,Mondovì, Bruno,Cirilli, Roberto,La Torre, Francesco
, p. 2071 - 2074 (2007/10/03)
A novel series of 1-acetyl-3-(4-hydroxy- and 2,4-dihydroxyphenyl)-5-phenyl-4,5-dihydro-(1H)-pyrazole derivatives 1 - 12 have been synthesized and investigated for the ability to selectively inhibit the activity of the A and B isoforms of monoamine oxidase
Synthesis and activity of a new series of chalcones as aldose reductase inhibitors
Severi, Fabio,Benvenuti, Stefania,Costantino, Luca,Vampa, Gabriella,Melegari, Michele,Antolini, Luciano
, p. 859 - 866 (2007/10/03)
A new series of chalcone derivatives has been synthesized and tested in vitro in order to assess their ability to inhibit aldose reductase enzyme (ALR2) and their specificity towards the target enzyme with respect to other oxidoreductases, such as aldehyde reductase, sorbitol dehydrogenase, and glutathione reductase. All the compounds display affinity for ALR2. The X-ray crystal structure of 1-(2,4-dihydroxyphenyl)-3-(2-methoxyphenyl)propen-1-one was determined.
Studies in cell suspension cultures of cassia didymobotrya. Part VI. The biotransformation of chalcones to aurones and auronols
Botta, Bruno,Delle Monache, Giuliano,De Rosa, Maria Cristina,Scurria, Rosalba,Vitali, Alberto,Vinciguerra, Vittorio,Menendez, Pilar,Misiti, Domenico
, p. 1415 - 1421 (2007/10/03)
Cell-free extracts derived from tissue cultures of Cassia didymobotrya, which previously had been reported to convert 4-hydroxychalcones to flavones and biflavanones, catalyze the biotransformation of 2-hydroxychalcones to aurones and auronols. The aurone
