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)

DOI: 10.1016/j.bmcl.2010.01.135

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Bioorganic and Medicinal Chemistry Letters p. 2321 - 2325 (2010)

Update date:2022-07-29

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Authors:

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 Yu, Ker

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Article abstract of DOI:10.1016/j.bmcl.2010.01.135

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

Full text of DOI:10.1016/j.bmcl.2010.01.135

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