Source:http://linkedlifedata.com/resource/pubmed/id/21388141
Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
7
|
pubmed:dateCreated |
2011-4-7
|
pubmed:abstractText |
Phosphatidylinositol 3-kinase ? (PI3K?) is an important regulator of intracellular signaling pathways, controlling remarkably diverse arrays of physiological processes. Because the PI3K pathway is frequently up-regulated in human cancers, the inhibition of PI3K? 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 PI3K? 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 PI3K? inhibitors. Representative derivatives showed good activity in cellular proliferation and apoptosis assays. Moreover, these inhibitors exhibited noteworthy antiangiogenic activity.
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
|
pubmed:month |
Apr
|
pubmed:issn |
1520-4804
|
pubmed:author | |
pubmed:issnType |
Electronic
|
pubmed:day |
14
|
pubmed:volume |
54
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
2455-66
|
pubmed:meshHeading |
pubmed-meshheading:21388141-Cell Line, Tumor,
pubmed-meshheading:21388141-Cell Proliferation,
pubmed-meshheading:21388141-Drug Design,
pubmed-meshheading:21388141-Enzyme Inhibitors,
pubmed-meshheading:21388141-Humans,
pubmed-meshheading:21388141-Models, Molecular,
pubmed-meshheading:21388141-Neovascularization, Pathologic,
pubmed-meshheading:21388141-Phosphatidylinositol 3-Kinases,
pubmed-meshheading:21388141-Protein Conformation,
pubmed-meshheading:21388141-Pyridines,
pubmed-meshheading:21388141-Signal Transduction,
pubmed-meshheading:21388141-Structure-Activity Relationship
|
pubmed:year |
2011
|
pubmed:articleTitle |
Design and synthesis of imidazopyridine analogues as inhibitors of phosphoinositide 3-kinase signaling and angiogenesis.
|
pubmed:affiliation |
Department of Chemistry, Korea Advanced Institute of Science and Technology, Daejeon 305-701, Korea.
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|