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Structure-based design of thienobenzoxepin inhibitors of PI3-kinase.

Abstract：

: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 xenograft model.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Staben ST,Siu M,Goldsmith R,Olivero AG,Do S,Burdick DJ,Heffron TP,Dotson J,Sutherlin DP,Zhu BY,Tsui V,Le H,Lee L,Lesnick J,Lewis C,Murray JM,Nonomiya J,Pang J,Prior WW,Salphati L,Rouge L,Sampath D,Sideris S,

doi

10.1016/j.bmcl.2011.04.124

subject

Has Abstract

pub_date

2011-07-01 00:00:00

pages

4054-8

issue

13

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)00594-4

journal_volume

21

pub_type

杂志文章

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