title: Development of N-4,6-pyrimidine-N-alkyl-N'-phenyl ureas as orally active inhibitors of lymphocyte specific tyrosine kinase.
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.
authors: Procter & Gamble Pharmaceuticals, Health Care Research Center, 8700 Mason-Montgomery Rd. Mason, OH 45040, USA.
authors: Jennifer A
authors: JA
authors: Maier
authors: Todd A
authors: TA
authors: Brugel
authors: Mark
authors: M
authors: Sabat
authors: Adam
authors: A
authors: Golebiowski
authors: Matthew J
authors: MJ
authors: Laufersweiler
authors: John C
authors: JC
authors: VanRens
authors: Corey R
authors: CR
authors: Hopkins
authors: Biswanath
authors: B
authors: De
authors: Lily C
authors: LC
authors: Hsieh
authors: Kimberly K
authors: KK
authors: Brown
authors: Vijayasurian
authors: V
authors: Easwaran
authors: Michael J
authors: MJ
authors: Janusz