Title of article
Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: Synthesis and SAR studies
Author/Authors
Xiaodong Lin، نويسنده , , Jeremy M. Murray، نويسنده , , Alice C. Rico، نويسنده , , Michael X. Wang، نويسنده , , Daniel T. Chu، نويسنده , , Yasheen Zhou، نويسنده , , Merci Del Rosario، نويسنده , , Susan Kaufman، نويسنده , , Sylvia Ma، نويسنده , , Eric Fang، نويسنده , , Kenneth Crawford، نويسنده , , A.B. Jefferson، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
6
From page
4163
To page
4168
Abstract
A series of 2-pyrimidyl-5-amidothiophenes has been synthesized and evaluated for AKT inhibition. SAR studies resulted in potent inhibitors of AKT with IC50 values as low as single digit nanomolar as represented by compound 2aa. Compound 2aa showed cellular activity including antiproliferation and downstream target modulation. Selectivity profile is described. A co-crystal of 2aa with PKA is determined and discussed.
Keywords
Protein Kinase B/Akt , kinase inhibitor , Substituted pyrimidine , cancer
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797154
Link To Document