110235-26-2Relevant academic research and scientific papers
Synthesis and structure-activity relationship study of triazine-based inhibitors of the DNA binding of NF-κB
Fujii, Shinya,Kobayashi, Takanobu,Nakatsu, Aki,Miyazawa, Hiroshi,Kagechika, Hiroyuki
, p. 700 - 708 (2014/08/05)
Nuclear transcription factor nuclear factor-kappa B (NF-κB) has diverse pathophysiological functions, and NF-κ B inhibitors are considered to be candidates for multiple therapeutic applications. We previously reported a novel triazine-based NF-κB inhibitor, 2-anilino-4,6-dichloro-1,3,5- triazine (NI241), that directly inhibits DNA binding of NF-κB. Here, we report synthesis of a series of triazine derivatives and evaluation of their structure-activity relationships for NF-κB inhibition. We found that 2-amino-4,6-dichloro-1,3,5-triazine substructure is essential for the inhibitory activity of the lead compound NI241, and modification of NI241 by introduction of an m-methoxy substituent on the phenyl ring afforded the more potent derivative 28. The structure-activity relationships identified in this study suggested a possible mechanism of irreversible NF-κB inhibition by NI241, and should be helpful in the design of other NF-κB inhibitors.
Pyrimidine derivative, process for preparing same and agricultural or horticultural fungicidal composition containing same
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, (2008/06/13)
Disclosed are pyrimidine derivatives represented by general formula STR1 wherein Z1 represents an alkynyl group, an alkenyl group, an alkoxy group, an alkenyloxy group, or an alkynyloxy group which may be substituted with a halogen atom, and Z2 represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, or a group of the formula STR2 where Z3 represents a hydrogen atom or a methyl group; or its salt; and processes for preparing same. Also, agricultural or horticultural compositions containing the pyrimidine derivatives as active ingredient are disclosed, which show high controlling activities for cucumber gray mold (Botrytis cinerea), cucumber downey mildew (Pseudoperonospora cubensis), Alternaria sooty spot of Chinese mustard (Alternaria brassicicola), rice blast (Pyricularia oryzae), etc.
