904745-61-5Relevant academic research and scientific papers
Design, synthesis, and evaluation of novel porcupine inhibitors featuring a fused 3-ring system based on the ‘reversed’ amide scaffold
Xu, Zhixiang,Xu, Xiangxiang,O'Laoi, Ruadhan,Ma, Haikuo,Zheng, Jiyue,Chen, Shuaishuai,Luo, Lusong,Hu, Zhilin,He, Sudan,Li, Jiajun,Zhang, Hongjian,Zhang, Xiaohu
, p. 5861 - 5872 (2016)
The Wnt signaling pathway is an essential signal transduction pathway which leads to the regulation of cellular processes such as proliferation, differentiation and migration. Aberrant Wnt signaling is known to have an association with multiple cancers. Porcupine is an enzyme that catalyses the addition of palmitoleate to a serine residue in Wnt proteins, a process which is required for the secretion of Wnt proteins. Here we report the synthesis and structure–activity-relationship of the novel porcupine inhibitors based on a ‘reversed’ amide scaffold. The leading compound 53 was as potent as the clinical compound LGK974 in a cell based STF reporter gene assay. Compound 53 potently inhibited the secretion of Wnt3A, therefore was confirmed to be a porcupine inhibitor. Furthermore, compound 53 showed excellent chemical and plasma stabilities. However, the clearance of compound 53 in liver microsomal tests was moderate to high, and the solubility of compound 53 was suboptimal. Collective efforts toward further optimization of this novel tricyclic template to develop better porcupine inhibitors will be subsequently undertaken and reported in due course.
Heterocyclic compound with Wnt signal path inhibitory activity and application thereof
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Paragraph 0263; 0264; 0265, (2016/10/08)
The invention provides a heterocyclic compound with Wnt signal path inhibitory activity. The heterocyclic compound and chemically acceptable salt, isotope, isomer and a crystal structure thereof are provided with a structure shown as the general formula I (see the formula in the description). The invention further provides application of the heterocyclic compound with the Wnt signal path inhibitory activity. The heterocyclic compound with the Wnt signal path inhibitory activity serves as effective antagonist of a Wnt signal path, and can be used for treating or preventing diseases caused by abnormity of the Wnt signal path.
METHOD FOR PRODUCING PEST CONTROLLING AGENT
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Paragraph 0120, (2014/07/09)
To supply a derivative having a 2-acyliminopyridine structure and being represented by the following formula (I) in an amount required as a pest control agent stably and at a low cost, provided is a method comprising the steps of: acylating an amino group at position 2 of a compound represented by formula (A) by use of an acylating agent, to thereby produce a compound represented by formula (B); and further alkylating a nitrogen atom at position 1 of the compound represented by formula (B): [where Ar represents a phenyl group or a 5-to 6-membered heterocycle, R1 represents a C1-6 alkyl group, and Y represents a hydrogen atom; a halogen atom; a hydroxyl group; a C1-6 alkyl group which may be substituted with a halogen atom; a C1-6 alkyloxy group which may be substituted with a halogen atom; a cyano group; a formyl group; or a nitro group].
PEST CONTROL AGENT
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Paragraph 0397; 0398, (2013/06/27)
Specific amine derivatives have been found to possess excellent activities as pest control agents.
Pest control composition including novel iminopyridine derivate
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Paragraph 0240; 0241, (2013/09/12)
Provided is a pest control composition containing a novel iminopyridine derivative and other pest control agents. Provided is a pest control composition containing an iminopyridine derivative represented by the following Formula (I) and at least one of other pest control agents: [in the formula, Ar represents a 5- to 6-membered heterocycle which may be substituted, A represents a heterocycle having a 5- to 10-membered unsaturated bond including one or more nitrogen atoms, and has an imino group substituted with an R group at a position adjacent to the nitrogen atom present on the cycle, Y represents hydrogen, halogen and the like, and R represents any one of groups represented by the following Formulae (a) to (e), (y) or (z)].
Nitrogen-containing hetercyclic derivate having 2-imino group and pest control agent including the same
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Paragraph 0231; 0232, (2013/09/12)
Provided is a nitrogen-containing heterocyclic derivative having a 2-imino group, which is represented by the following Formula (I). [in the formula, Ar represents a phenyl group which may be substituted, a 5- to 6-membered heterocycle which may be substituted, or a 4- to 10-membered heterocycloalkyl group, A represents a heterocycle having a 5- to 10-membered unsaturated bond including one or more nitrogen atoms, and has an imino group substituted with an R group at a position adj acent to the nitrogen atom present on the cycle, Y represents a hydrogen atom, a halogen atom, a hydroxyl group, a C1 to C6 alkyl group which may be substituted with a halogen atom, a C1 to C6 alkyloxy group which may be substituted with a halogen atom, a cyano group, or a nitro group, and R represents any one of groups represented by the following Formulae (a) to (e), (y) or (z).]
INSECTICIDAL N-SUBSTITUTED (HETEROARYL)ALKYL SULFILMINES
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Page/Page column 25, (2008/06/13)
N -Substituted (heteroaryl)alkyl sulfilimines are effective at controlling insects.
Multi-substituted pyridyl sulfoximines and their use as insecticides
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Page/Page column 8, (2008/12/04)
Multi-substituted pyridyl sulfoximines are useful as insecticides.
