6272-26-0Relevant articles and documents
Flavone inspired discovery of benzylidenebenzofuran-3(2H)-ones (aurones) as potent inhibitors of human protein kinase CK2
Bdzhola, V. G.,Bilokin, Y. V.,Borysenko, I. P.,Lukashov, S. S.,Protopopov, M. V.,Prykhod'ko, A. O.,Starosyla, S. A.,Vdovin, V. S.,Yarmoluk, S. M.
supporting information, (2020/07/21)
In this work, we describe the design, synthesis and SAR studies of 2-benzylidenebenzofuran-3-ones (aurones), a new family of potent inhibitors of CK2. A series of aurones have been synthesized. These compounds are structurally related to the synthetic flavones and showed nanomolar activities towards CK2. Biochemical tests revealed that 20 newly synthesized compounds inhibited CK2 with IC50 values in the nanomolar range. Further property-based optimization of aurones was performed, yielding a series of CK2 inhibitors with enhanced lipophilic efficiency. The most potent compound 12m (BFO13) has CLipE = 4.94 (CLogP = 3.5; IC50 = 3.6 nM) commensurable with the best known inhibitors of CK2.
PD-1/PD-L1 small-molecule inhibitor and preparation method and application thereof
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Paragraph 0221; 0226; 0227; 0228, (2019/05/08)
The invention discloses a PD-1/PD-L1 small-molecule inhibitor and a preparation method and application thereof. Specifically, the invention discloses a compound with the structure shown in the formulaL, a stereoisomer or a tautomer thereof, or pharmaceutically acceptable salts or hydrates or solvates thereof, and please see the specification for specific definitions. The compound has excellent effects for restraining PD-1/PD-L1. Please see the specification for the formula.
Aurones as new porcine pancreatic α-amylase inhibitors
Roshanzamir, Khashayar,Kashani-Amin, Elaheh,Ebrahim-Habibi, Azadeh,Navidpour, Latifeh
, p. 333 - 340 (2019/06/20)
Background: Aurones, (Z)-2-benzylidenebenzofuran-3-one derivatives, are naturally-occurring structural isomers of flavones, with promising pharmacological potential. Methods: In this study, the structural requirements for the inhibition of porcine pancreatic α-amylase by hydroxylated or methoxylated aurone derivatives were investigated by assessing their in vitro biological activities against porcine pancreatic α-amylase. Results: The structure-activity relationship of these inhibitors based on both in vitro and in silico findings showed that the hydrogen bonds between the OH groups of the A or B ring of (Z)-benzylidenebenzofuran-3-one derivatives and the catalytic residues of the binding site are crucial for their inhibitory activities. Conclusion: It seems that the OH groups in aurones inhibit α-amylase in a manner similar to that of OH groups in flavones and flavonols.