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PDBsum entry 3dbs
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References listed in PDB file
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Key reference
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Title
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The identification of 2-(1h-Indazol-4-Yl)-6-(4-Methanesulfonyl-Piperazin-1-Ylmethyl)-4-Morpholin-4-Yl-Thieno[3,2-D]pyrimidine (gdc-0941) as a potent, Selective, Orally bioavailable inhibitor of class i pi3 kinase for the treatment of cancer .
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Authors
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A.J.Folkes,
K.Ahmadi,
W.K.Alderton,
S.Alix,
S.J.Baker,
G.Box,
I.S.Chuckowree,
P.A.Clarke,
P.Depledge,
S.A.Eccles,
L.S.Friedman,
A.Hayes,
T.C.Hancox,
A.Kugendradas,
L.Lensun,
P.Moore,
A.G.Olivero,
J.Pang,
S.Patel,
G.H.Pergl-Wilson,
F.I.Raynaud,
A.Robson,
N.Saghir,
L.Salphati,
S.Sohal,
M.H.Ultsch,
M.Valenti,
H.J.Wallweber,
N.C.Wan,
C.Wiesmann,
P.Workman,
A.Zhyvoloup,
M.J.Zvelebil,
S.J.Shuttleworth.
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Ref.
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J Med Chem, 2008,
51,
5522-5532.
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PubMed id
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Abstract
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Phosphatidylinositol-3-kinase (PI3K) is an important target in cancer due to the
deregulation of the PI3K/ Akt signaling pathway in a wide variety of tumors. A
series of thieno[3,2-d]pyrimidine derivatives were prepared and evaluated as
inhibitors of PI3 kinase p110alpha. The synthesis, biological activity, and
further profiling of these compounds are described. This work resulted in the
discovery of 17, GDC-0941, which is a potent, selective, orally bioavailable
inhibitor of PI3K and is currently being evaluated in human clinical trials for
the treatment of cancer.
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