932708-08-2Relevant articles and documents
Substituted 3-benzylcoumarins as allosteric MEK1 inhibitors: Design, synthesis and biological evaluation as antiviral agents
Wang, Chao,Zhang, Hao,Xu, Fengrong,Niu, Yan,Wu, Yun,Wang, Xin,Peng, Yihong,Sun, Jing,Liang, Lei,Xu, Ping
, p. 6057 - 6091 (2013)
In order to find novel antiviral agents, a series of allosteric MEK1 inhibitors were designed and synthesized. Based on docking results, multiple optimizations were made on the coumarin scaffold. Some of the derivatives showed excellent MEK1 binding affinity in the appropriate enzymatic assays and displayed obvious inhibitory effects on the ERK pathway in a cellular assay. These compounds also significantly inhibited virus (EV71) replication in HEK293 and RD cells. Several compounds showed potential as agents for the treatment of viral infective diseases, with the most potent compound 18 showing an IC 50 value of 54.57 nM in the MEK1 binding assay.
Agents and methods for treating ischemic and other diseases
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Page/Page column 138; 139, (2016/06/01)
This invention relates to compounds that modulate TRPM7 protein activity and use of the same for treatment or prophylaxis of ischemia, cancer, pain or glaucoma.
QUINOLINES AND THEIR THERAPEUTIC USE
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Page/Page column 79, (2008/06/13)
Compounds of formula [1] are CRTH2 antagonists, useful in the treatment of conditions having an inflammatory component; in which: R1, R2, R3, R4 and R5 are independently hydrogen, C1-C6alkyl, C1- C6fluoroalkyl, cyclopropyl, halo, -S(O)nR6, -SO2NR7R8, -NR7R8, -NR7C(O)R6, -CO2R7, -C(O)NR7R8, -C(O)R6, -NO2, -CN or a group -OR9; wherein each R6 is independently C1-C6alkyl, C1-C6fluoroalkyl, cycloalkyl, aryl, or heteroaryl; R7, R8 are independently C1-C6alkyl, C1-C6fluoroalkyl, cycloalkyl, cycloalkyl-(C1-C6alkyl)-, aryl, heteroaryl or hydrogen; R9 is hydrogen, C1-C6alkyl, C1-C6fluoroalkyl, cycloalkyl, cylcoalkyl-(C1-C6alkyl)-, or a group -SO2R6; A is -CHR10-, -C(O)-, -S(O)n-, -0-, or -NR10- wherein n is an integer from 0-2 and R10 is hydrogen, C1-C3alkyl, or C1-C6fluoroalkyl group; B is a direct bond, or a divalent radical selected from -CH2-, -CH2CH2-, -CHR11-, -CR11R12-, -CH2CHR11-, -CH2CR11R12-, -CHR11CHR12-, and divalent radicals of formula -(CR11R12)P-Z- wherein Z is attached to the ring carrying R1, R2 and R3; wherein R11 is C1-C3alkyl, cyclopropyl, C1-C6fluoroalkyl; R12 is methyl or fluoromethyl; p is independently 1 or 2; and Z is -0-, -NH-, or -S(O)n-, wherein n is an integer from 0-2; X is a carboxylic acid, tetrazole, 3-hydroxyisoxazole, hydroxamic acid, phosphinate, phosphonate, phosphonamide, or sulfonic acid group, or a group of formula C(=O)NHSO2R6or SO2NHC(=O)R6; and Y is aryl, heteroaryl, aryl-fused- heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused-heterocycloalkyl or aryl-fused-cycloalkyl group.