Design and Synthesis of Imidazopyridine Analogues as Inhibitors of Phosphoinositide 3-Kinase Signaling and Angiogenesis

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Phosphatidylinositol 3-kinase alpha (P13K alpha) is an important regulator of intracellular signaling pathways, controlling remarkably diverse arrays of physiological processes. Because the P13K pathway is frequently up-regulated in human cancers, the inhibition of P13K alpha can be a promising approach to cancer therapy. In this study, we have designed and synthesized a new series of imidazo[1,2-a]pyridine derivatives as P13K alpha inhibitors through the fragment-growing strategy. By varying groups at the 3- and 6-positions of imidazo[1,2-a]pyridines, we studied the structure-activity relationships (SAR) profiles and identified a series of potent P13K alpha inhibitors. Representative derivatives showed good activity in cellular proliferation and apoptosis assays. Moreover, these inhibitors exhibited note-worthy antiangiogenic activity.
Publisher
AMER CHEMICAL SOC
Issue Date
2011-04
Language
English
Article Type
Article
Keywords

ENDOTHELIAL GROWTH-FACTOR; IN-VIVO; CANCER; POTENT; IDENTIFICATION; MUTATIONS; DISCOVERY; RAPAMYCIN; ISOFORM; PATHWAY

Citation

JOURNAL OF MEDICINAL CHEMISTRY, v.54, no.7, pp.2455 - 2466

ISSN
0022-2623
DOI
10.1021/jm101582z
URI
http://hdl.handle.net/10203/97883
Appears in Collection
CH-Journal Papers(저널논문)
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