Structure-activity relationships of quinazoline derivatives: dual-acting compounds with inhibitory activities toward both TNF-alpha production and T cell proliferation

  • Bioorg Med Chem Lett. 2001 Feb 26;11(4):545-8. doi: 10.1016/s0960-894x(00)00718-6.
M Tobe  1 ,  Y Isobe ,  H Tomizawa ,  M Matsumoto ,  F Obara ,  T Nagasaki ,  H Hayashi
Affiliations
  • 1. Pharmaceuticals and Biotechnology Laboratory, Japan Energy Corporation, Saitama, Japan.
PMID: 11229767 DOI: 10.1016/s0960-894x(00)00718-6
Abstract

We synthesized 4-chlorophenethylaminoquinazoline derivatives and evaluated their inhibitory activities toward both TNF-alpha production and T cell proliferation responses. Compound 2f, containing a piperazine ring at the C(7)-position of the quinazoline ring, exhibited more potent inhibitory activities toward both than the lead compound la. A smaller N-substituent in the piperazine ring was required for inhibition of TNF-alpha production.