76434-54-3Relevant articles and documents
Antibacterial agent as well as synthetic method and application thereof
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Paragraph 0046; 0048; 0049; 0056; 0063, (2017/10/07)
The invention relates to an antibacterial agent as well as a synthetic method and application thereof and belongs to the field of biotechnology. The antibacterial agent is 3,3',4',5,5'-pentahydroxyflavanone. The synthetic method comprises the following st
Hydroxylated chalcones with dual properties: Xanthine oxidase inhibitors and radical scavengers
Hofmann, Emily,Webster, Jonathan,Do, Thuy,Kline, Reid,Snider, Lindsey,Hauser, Quintin,Higginbottom, Grace,Campbell, Austin,Ma, Lili,Paula, Stefan
, p. 578 - 587 (2016/02/09)
In this study, we evaluated the abilities of a series of chalcones to inhibit the activity of the enzyme xanthine oxidase (XO) and to scavenge radicals. 20 mono- and polyhydroxylated chalcone derivatives were synthesized by Claisen-Schmidt condensation reactions and then tested for inhibitory potency against XO, a known generator of reactive oxygen species (ROS). In parallel, the ability of the synthesized chalcones to scavenge a stable radical was determined. Structure-activity relationship analysis in conjunction with molecular docking indicated that the most active XO inhibitors carried a minimum of three hydroxyl groups. Moreover, the most effective radical scavengers had two neighboring hydroxyl groups on at least one of the two phenyl rings. Since it has been proposed previously that XO inhibition and radical scavenging could be useful properties for reduction of ROS-levels in tissue, we determined the chalcones' effects to rescue neurons subjected to ROS-induced stress created by the addition of β-amyloid peptide. Best protection was provided by chalcones that combined good inhibitory potency with high radical scavenging ability in a single molecule, an observation that points to a potential therapeutic value of this compound class.
Identification and initial SAR of silybin: An Hsp90 inhibitor
Zhao, Huiping,Brandt, Gary E.,Galam, Lakshmi,Matts, Robert L.,Blagg, Brian S.J.
scheme or table, p. 2659 - 2664 (2011/06/22)
Through Hsp90-dependent firefly luciferase refolding and Hsp90-dependent heme-regulated eIF2α kinase (HRI) activation assays, silybin was identified as a novel Hsp90 inhibitor. Subsequently, a library of silybin analogues was designed, synthesized and evaluated. Initial SAR studies identified the essential, non-essential and detrimental functionalities on silybin that contribute to Hsp90 inhibition.
Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 1
Masubuchi, Miyako,Kawasaki, Ken-ichi,Ebiike, Hirosato,Ikeda, Yoshihiko,Tsujii, Shinji,Sogabe, Satoshi,Fujii, Toshihiko,Sakata, Kiyoaki,Shiratori, Yasuhiko,Aoki, Yuko,Ohtsuka, Tatsuo,Shimma, Nobuo
, p. 1833 - 1837 (2007/10/03)
Potent and selective Candida albicans N-myristoyltransferase (CaNmt) inhibitors have been identified through optimization of a lead compound 1 discovered by random screening. The inhibitor design is based on the crystal structure of the CaNmt complex with compound (S)-3 and structure-activity relationships (SARs) have been clarified. Modification of the C-4 side chain of 1 has led to the discovery of a potent and selective CaNmt inhibitor 11 (RO-09-4609), which exhibits antifungal activity against C. albicans in vitro.
A NOVEL AND EFFICIENT SYNTHESIS OF 5-SUBSTITUTED AND 5,6-DISUBSTITUTED 4-METHYLCOUMARINS USING ORGANOCERIUM(III) REAGENTS
Nagasawa, Kazuo,Kanbara, Hajime,Matsushita, Kazuya,Ito, Keiichi
, p. 6477 - 6480 (2007/10/02)
Addition of organocerium(III) reagent, Cl2CeCH2COOt-Bu, to the appropriate ortho-methoxymethoxyacetophenones followed by acid treatment gives 5-substituted and 5,6-disubstituted 4-methylcoumarins in excellent yields.