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Discovery of novel phenoxazinone derivatives as DKK1/LRP6 interaction inhibitors: Synthesis, biological evaluation and structure-activity relationships.

Abstract：

:Amino derivatives of NCI8642 were synthesized and evaluated as inhibitors of DKK1/LRP6 interactions. The new inhibitors were able to activate the Wnt signaling pathway as indicated by the increased levels of β-catenin, and decrease the DKK1-induced Tau phosphorylation at serine 396.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Thysiadis S,Mpousis S,Avramidis N,Katsamakas S,Balomenos A,Remelli R,Efthimiopoulos S,Sarli V

doi

10.1016/j.bmc.2016.01.025

subject

Has Abstract

pub_date

2016-03-01 00:00:00

pages

1014-22

issue

5

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(16)30025-6

journal_volume

24

pub_type

杂志文章

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