An article Design, synthesis and biological evaluation of new embelin derivatives as CK2 inhibitors WOS:000512762900040 published article about PROTEIN-KINASE CK2; EMERGING ROLE; ASSAY; SURVIVAL; DOCKING; GLIDE; WNT in [Oramas-Royo, Sandra; Amesty, Angel; Martin-Acosta, Pedro; Estevez-Braun, Ana] Univ La Laguna, Dept Quim Organ, Inst Univ Bioorgan Antonio Gonzalez, Avda Astrofis Francisco Sanchez 2, Tenerife 38206, Spain; [Haidar, Samer; Aichele, Dagmar; Jose, Joachim] Westfalische Wilhelms Univ Munster, Inst Pharmazeut & Med Chem, PharmaCampus,Corrensstr 48, D-48149 Munster, Germany; [Haidar, Samer] Damascus Univ, Fac Pharm, 17 April St, Damascus, Syria; [Feresin, Gabriela; Tapia, Alejandro] Univ Nacl San Juan, Inst Ciencias Basicas, Inst Biotecnol, Av Libertador Gen San Martin 1109 O, RA-5400 San Juan, Argentina in 2020.0, Cited 33.0. Recommanded Product: 500-22-1. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1
A new series of furan embelin derivatives was synthesized and characterized as ATP-competitive CK2 inhibitors. The new compounds were efficiently synthesized using a multicomponent approach from embelin (1), aldehydes and isonitriles through a Knoevenagel condensation/Michael addition/heterocyclization. Several compounds with inhibitory activities in the low micromolar or even submicromolar were identified. The most active derivative was compound 4l (2-(tert-butylamino)-3-(furan-3-yl)-5-hydroxy-6-undecylbenzofuran-4,7-dione) with an IC50 value of 0.63 mu M. It turned out to be an ATP competitive CK2 inhibitor with a K-i value determined to be 0.48 mu M. Docking studies allowed the identification of key ligand-CK2 interactions, which could help to further optimize this family of compounds as CK2 inhibitors.
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Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem