Imidazo[1,5-a]pyrazines: Orally efficacious inhibitors of mTORC1 and mTORC2

DOI: 10.1016/j.bmcl.2011.01.139

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 2092 - 2097 (2011)

Update date:2022-08-05

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Authors:

Crew, Andrew P.

Bhagwat, Shripad V.

Dong, Hanqing

Bittner, Mark A.

Chan, Anna

Chen, Xin

Coate, Heather

Cooke, Andrew

Gokhale, Prafulla C.

Honda, Ayako

Jin, Meizhong

Kahler, Jennifer

Mantis, Christine

Mulvihill, Mark J.

Tavares-Greco, Paula A.

Volk, Brian

Wang, Jing

Werner, Douglas S.

Arnold, Lee D.

Pachter, Jonathan A.

Wild, Robert

Gibson, Neil W.

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Article abstract of DOI:10.1016/j.bmcl.2011.01.139

The discovery and optimization of a series of imidazo[1,5-a]pyrazine inhibitors of mTOR is described. HTS hits were optimized for potency, selectivity and metabolic stability to provide the orally bioavailable proof of concept compound 4c that demonstrate

Full text of DOI:10.1016/j.bmcl.2011.01.139

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