Synthesis and immunostimulatory activity of 8-substituted amino 9-benzyladenines as potent Toll-like receptor 7 agonists

  • Bioorg Med Chem Lett. 2006 Sep 1;16(17):4559-63. doi: 10.1016/j.bmcl.2006.06.017.
Guangyi Jin  1 ,  Christina C N Wu ,  Rommel I Tawatao ,  Michael Chan ,  Dennis A Carson ,  Howard B Cottam
Affiliations
  • 1. Moores Cancer Center, University of California, San Diego, La Jolla, 92093-0820, USA.
PMID: 16784848 DOI: 10.1016/j.bmcl.2006.06.017
Abstract

Several 9-benzyl adenine derivatives bearing various substituted amines at the 8-position have been prepared and evaluated for interferon induction in peripheral blood mononuclear cells (PBMC) from healthy human donors. The 8-bromoadenine derivative 5 was used as a versatile intermediate for all substitutions. The most active 8-substituted amino compound was found to be the 8-morpholinoethylamino derivative 19 which had an EC(50) in the submicromolar range.