685853-10-5Relevant academic research and scientific papers
Design, synthesis and biological evaluation of 2-aminopyrimidinones and their 6-aza-analogs as a new class of CK2 inhibitors
Chekanov, Maksym O.,Ostrynska, Olga V.,Tarnavskyi, Sergii S.,Synyugin, Anatoliy R.,Briukhovetska, Nadiia V.,Bdzhola, Volodymyr G.,Pashenko, Alexander E.,Fokin, Andrey A.,Yarmoluk, Sergiy M.
, p. 639 - 646 (2014)
In order to find the new potent CK2 inhibitors the 60 derivatives of 2-aminopyrimidinone and their 6-aza-substituted analogs were synthesized and tested in vitro. Among them, the most efficient inhibitor 2-hydroxy-5-[4-(4-methoxyphehyl)-6-oxo-1,6-dihydropyrimidin-2-ylamino] benzoic acid was identified (IC50=1.1μM). The structure - activity relationship study of newly synthesized derivatives was carried out and their binding mode with adenosine triphosphate-acceptor site of CK2 was proposed.
