- Discovery of 1,8-disubstituted-[1,2,3]triazolo[4,5-c]quinoline derivatives as a new class of Hippo signaling pathway inhibitors
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Inhibitors of the Hippo signaling pathway have been demonstrated to have a potential clinical application in cases such as tissue repair and organ regeneration. However, there is a lack of potent Hippo pathway inhibitors at present. Herein we report the discovery of a series of 1,8-disubstituted-[1,2,3]triazolo[4,5-c]quinoline derivatives as a new class of Hippo pathway inhibitors by utilizing a cell line-based screening model (A549-CTGF). Structure-activity relationship (SAR) of these compounds was also discussed. The most potent compound in the A549-CTGF cell assay, 11g, was then evaluated by real-time PCR and immunofluorescence assays. Overall, this study provides a starting point for later drug discovery targeting the Hippo signaling pathway.
- Chen, Pei,Li, L.,Lin, Guifeng,Qiao, Jingxin,Xia, A.,Xiang, Z.,Yang, Shengyong,Zhang, Guo
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- PYRROLOPYRIDINE INHIBITORS OF KINASES
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The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1a, R1b, R1c, X, and Y are defined in the description. The present invention relates also to compositions containing sa
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Page/Page column 30
(2011/02/18)
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- PHTHALAZIN-(2H)-ONE INHIBITORS OF KINASES
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The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1a, R1b, R1c, X, Y, Z, n, and m are defined in the description. The present invention relates also to compositions cont
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Page/Page column 22
(2011/10/31)
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- PYRROLOPYRAZINONE INHIBITORS OF KINASES
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The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1a, R1b, R1c, X, Y, Z, n, and m are defined in the description. The present invention relates also to compositions cont
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Page/Page column 35
(2011/10/31)
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- PYRIDINONYL PDK1 INHIBITORS
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The present invention provides pyridinonyl PDKl inhibitors and methods of treating cancer using the same.
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- INHIBITORS OF Akt ACTIVITY
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Invented are novel thiophene compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
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Page/Page column 53
(2010/11/27)
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- Synthesis of 2-amino-4-(7-azaindol-3-yl)pyrimidines as cyclin dependent kinase 1 (CDK1) inhibitors
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A novel series of 2-amino-4-(7-azaindol-3-yl)pyrimidines was discovered as cyclin dependent kinase 1 (CDK1) inhibitors. The core structure was synthesized via Pd(II) catalyzed coupling reaction. A number of analogues showed good potency for CDK1 and exhib
- Huang, Shenlin,Li, Ronghua,Connolly, Peter J.,Emanuel, Stuart,Middleton, Steven A.
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p. 4818 - 4821
(2007/10/03)
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- PYRIMIDINYL SUBSTITUTED FUSED-PYRROLYL COMPOUNDS USEFUL IN TREATING KINASE DISORDERS
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The present invention provides pyrimidinyl substituted fused-pyrrolyl compounds of Formula (I) and pharmaceutical compositions comprising the compounds and methods of synthesis and use thereof. The compounds are kinase inhibitors useful in treating or ameliorating a kinase mediated, angiogenesis-mediated or hyperproliferative disorder. The invention thus also provides a therapeutic or prophylactic method of use for the compounds and/or pharmaceutical compositions to treat such disorders.
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Page/Page column 62
(2010/11/30)
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