Bioorganic and Medicinal Chemistry Letters p. 4054 - 4058 (2011)
Update date:2022-08-03
Topics:
Staben, Steven T.
Siu, Michael
Goldsmith, Richard
Olivero, Alan G.
Do, Steven
Burdick, Daniel J.
Heffron, Timothy P.
Dotson, Jenna
Sutherlin, Daniel P.
Zhu, Bing-Yan
Tsui, Vickie
Le, Hoa
Lee, Leslie
Lesnick, John
Lewis, Cristina
Murray, Jeremy M.
Nonomiya, Jim
Pang, Jodie
Prior, Wei Wei
Salphati, Laurent
Rouge, Lionel
Sampath, Deepak
Sideris, Steve
Wiesmann, Christian
Wu, Ping
Starting from thienobenzopyran HTS hit 1, co-crystallization, molecular modeling and metabolic analysis were used to design potent and metabolically stable inhibitors of PI3-kinase. Compound 15 demonstrated PI3K pathway suppression in a mouse MCF7 xenogra
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