Title of article
Development of N-4,6-pyrimidine-N-alkyl-N′-phenyl ureas as orally active inhibitors of lymphocyte specific tyrosine kinase
Author/Authors
Jennifer A. Maier، نويسنده , , Todd A. Brugel، نويسنده , , Mark Sabat، نويسنده , , Adam Golebiowski، نويسنده , , Matthew J. Laufersweiler، نويسنده , , John C. VanRens، نويسنده , , Corey R. Hopkins، نويسنده , , Biswanath De، نويسنده , , Lily C. Hsieh، نويسنده , , Kimberly K. Brown، نويسنده , , Vijayasurian Easwaran، نويسنده , , Michael J. Janusz، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
5
From page
3646
To page
3650
Abstract
A new class of lymphocyte specific tyrosine kinase (lck) inhibitors based on an N-4,6-pyrimidine-N-alkyl-N′-phenyl urea scaffold is described. Many of these compounds showed low-nanomolar inhibition of lck kinase activity as well as IL-2 synthesis from Jurkat cells. One of these analogs, 7i, was shown to be orally efficacious by in vivo testing in a rat adjuvant-induced arthritis study.
Keywords
Lck kinase , IL-2 cytokine , rheumatoid arthritis , Trisubstituted ureas
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797049
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