915118-70-6Relevant articles and documents
Design, synthesis, and biological evaluation of pyrimidine derivatives as potential inhibitors of human calcium/calmodulin-dependent protein kinase IV
Jameel, Ehtesham,Naz, Huma,Khan, Parvez,Tarique, Mohd.,Kumar, Jitendra,Mumtazuddin, Syed,Ahamad, Shahzaib,Islam, Asimul,Ahmad, Faizan,Hoda, Nasimul,Hassan, Md. Imtaiyaz
, p. 741 - 754 (2017)
Calcium/calmodulin-dependent protein kinase IV (CAMKIV) is a multifunctional Ser/Thr kinase, associated with cerebral hypoxia, cancer, and neurodegenerative diseases. Here, we report design, synthesis, and biological evaluation of seven pyrimidine-substituted novel inhibitors of CAMKIV. We successfully synthesized and extensively characterized (ESI-MS, 1H NMR, and 13C NMR studies) seven compounds that are showing appreciable binding affinity to the CAMKIV. Molecular docking and fluorescence binding studies revealed that compound 1 is showing very high binding free energy (ΔG?=??11.52?kcal/mol) and binding affinity (K?=?9.2?×?1010 m?1) to the CAMKIV. We further performed MTT assay to check the cytotoxicity and anticancer activity of these compounds. An appreciable IC50 (39?μm) value of compound 1 was observed on human hepatoma cell line and nontoxic till the 400?μm on human embryonic kidney cells. To ensure anticancer activity of all these compounds, we further performed propidium iodide assay to evaluate cell viability and DNA content during the cell cycle. We found that compound 1 is again showing a better anticancer activity on both human hepatoma and human embryonic kidney cell lines.
A N, 6 diphenyl pyrimidine -4 - amine Bcr - Abl inhibitor and its preparation method and application (by machine translation)
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Paragraph 0107-0110, (2017/04/28)
The invention discloses a N, 6 diphenyl pyrimidine - 4 - amine Bcr - Abl inhibitor and its preparation method and application, the structural formula of the inhibitor for the wherein R is a single substituent or double-substituent, substituent is alkyl or halogen; R1 As a single substituent or double-substituent, substituent is alkyl or halogen. The series of inhibitors in vitro ABL1 kinase restraining effects, and can inhibit the proliferation of tumor cells, can be used for anti-tumor pharmaceutical preparation, in particular CML (chronic granulocytic leukemia) drug. The invention provides N, 6 diphenyl pyrimidine - 4 - amine Bcr - Abl inhibitor preparation method, raw materials are apt, mild reaction conditions, the reaction process is simple in operation, reagent used and cheap. (by machine translation)
Library synthesis of cardiomyogenesis inducing compounds using an efficient two-step-one-flow process
Sch?n, Michael,Dreier, Dominik,Schnürch, Michael,Mihovilovic, Marko D.
, p. 523 - 532 (2016/03/19)
Within this work we telescoped a batch laboratory scale synthesis towards a two-step-one-flow process to synthesize cardiomyogenesis inducing compounds (4,6-diaminopyrimidines) in continuous manner. Special attention was put on a quick and robust screenin
