Structure-guided discovery of a novel, potent, and orally bioavailable 3,5-dimethylisoxazole aryl-benzimidazole BET bromodomain inhibitor.

David Sperandio, Vangelis Aktoudianakis,Kerim Babaoglu,Xiaowu Chen,Kristyna Elbel,Gregory Chin,Britton Corkey,Jinfa Du, Bob Jiang,Tetsuya Kobayashi,Richard Mackman,Ruben Martinez,Hai Yang,Jeff Zablocki,Saritha Kusam, Kim Jordan,Heather Webb,Jamie G Bates,Latesh Lad,Michael Mish,Anita Niedziela-Majka,Sammy Metobo,Annapurna Sapre,Magdeleine Hung, Debi Jin,Wanchi Fung,Elaine Kan, Gene Eisenberg, Nate Larson, Zachary E R Newby,Eric Lansdon, Chin Tay,Richard M Neve,Sophia L Shevick,David G Breckenridge

Bioorganic & Medicinal Chemistry（2019）

引用 13|浏览15

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摘要

•The structure-guided discovery of a novel BET bromodomain inhibitor is disclosed.•The lead properties were optimized using in-vitro assays and in-vivo PK studies.•The lead compound reduced the in vivo tumor growth two xenograft models.

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关键词

Antitumor,BET proteins,Bromodomain inhibitor,Epigenetic readers

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