- Palladium Catalyzed Regioselective C4-Arylation and Olefination of Indoles and Azaindoles
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A convergent strategy for the synthesis of biologically relevant C4-substituted indole scaffolds was demonstrated using Pd(II)-catalyzed remote C?H functionalization of indoles and azaindoles. The reaction displays high regioselectivity for the C4-positio
- Thrimurtulu, Neetipalli,Dey, Arnab,Singh, Anurag,Pal, Kuntal,Maiti, Debabrata,Volla, Chandra M. R.
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supporting information
(2019/02/13)
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- 4-Substituted-7-azaindoles bearing a ureidobenzofuranone moiety as potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR)
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A series of 5-ureidobenzofuranones was discovered as potent and selective inhibitors of mTOR with good cellular activity. Molecular modeling studies revealed several hydrogen bond interactions of the ureido group with the enzyme at the ATP-binding site. Furthermore, modeling showed that the ureido group is best situated at C-5 of the benzofuranone. Syntheses of 4-ureido and 5-ureidobenzofuranones are presented.
- Tsou, Hwei-Ru,MacEwan, Gloria,Birnberg, Gary,Zhang, Nan,Brooijmans, Natasja,Toral-Barza, Lourdes,Hollander, Irwin,Ayral-Kaloustian, Semiramis,Yu, Ker
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supporting information; experimental part
p. 2259 - 2263
(2010/06/15)
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- 3-SUBSTITUTED-1H-INDOLE, 3-SUBSTITUTED-1H-PYRROLO[2,3-B]PYRIDINE AND 3-SUBSTITUTED-1H-PYRROLO[3,2-B]PYRIDINE COMPOUNDS, THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES
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The invention relates to 3-substituted-1H-indole, 3-substituted-1H-pyrrolo[2,3-b]pyridine, and 3-substituted-1H-pyrrolo[3,2-b]pyridine compounds of the Formula (I): or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.
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Page/Page column 121
(2010/04/06)
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- Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR)
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We discovered 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR). Since phenolic OH groups pose metabolic liability, one of th
- Tsou, Hwei-Ru,MacEwan, Gloria,Birnberg, Gary,Grosu, George,Bursavich, Matthew G.,Bard, Joel,Brooijmans, Natasja,Toral-Barza, Lourdes,Hollander, Irwin,Mansour, Tarek S.,Ayral-Kaloustian, Semiramis,Yu, Ker
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scheme or table
p. 2321 - 2325
(2010/08/22)
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- 3-SUBSTITUTED-1H-PYRROLO[2,3-B]PYRIDINE AND 3-SUBSTITUTED-1H-PYRROLO[3,2-B]PYRIDINE COMPOUNDS, THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES
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The invention relates to 3-substituted-1H-pyrrolo[2,3-b]pyridine, and 3-substituted-1H-pyrrolo[3,2-b]pyridine compounds of the Formula 1: or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.
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Page/Page column 36-37
(2009/12/23)
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