5037-70-7Relevant academic research and scientific papers
4-Substituted-7-azaindoles bearing a ureidobenzofuranone moiety as potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR)
Tsou, Hwei-Ru,MacEwan, Gloria,Birnberg, Gary,Zhang, Nan,Brooijmans, Natasja,Toral-Barza, Lourdes,Hollander, Irwin,Ayral-Kaloustian, Semiramis,Yu, Ker
scheme or table, p. 2259 - 2263 (2010/06/15)
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.
5-Ureidobenzofuranone indoles as potent and efficacious inhibitors of PI3 kinase-α and mTOR for the treatment of breast cancer
Zhang, Nan,Ayral-Kaloustian, Semiramis,Anderson, James T.,Nguyen, Thai,Das, Sasmita,Venkatesan, Aranapakam M.,Brooijmans, Natasja,Lucas, Judy,Yu, Ker,Hollander, Irwin,Mallon, Robert
scheme or table, p. 3526 - 3529 (2010/08/20)
A series of 5-ureidobenzofuran-3-one indoles as potent inhibitors of PI3Kα and mTOR has been developed. The best potency in cells was obtained when the urea group was extended to a 4-[2-(dimethylamino)ethyl]methylamino amidophenyl group. A 7-fluoro group
[a]-FUSED INDOLE COMPOUNDS, THEIR USE AS mTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES
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Page/Page column 19; 25, (2009/08/14)
The invention relates to [a]-fused indole compounds of the Formula II, or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein. The invention also relates to compositions comprising the compounds of Formula II, and methods for making and using the compounds.
Regioselective synthesis of tetrasubstituted pyrroles by 1,3-dipolar cycloaddition and spontaneous decarboxylation
Kim, Yongju,Kim, Jonghoon,Park, Seung Bum
supporting information; experimental part, p. 17 - 20 (2009/08/07)
We developed a novel regioselective synthesis of tetrasubstituted pyrroles via the classic 1,3-dipolar cycloaddition of α,β-unsaturated benzofuran-3(2H)-one and azlactones (1) followed by spontaneous decarboxylation. The complete regiochemical control of tetrasubstituted pyrroles was confirmed by the orthogonal synthesis of complementary regioisomers (7a and 7b) simply by using different azlactones (1a and 1b, respectively).
