Structure-activity relationship analysis of substituted 4-quinolinamines, antagonists of immunostimulatory CpG-oligodeoxynucleotides

L Strekowski; O Zegrocka; M Henary; M Say; M J Mokrosz; B M Kotecka; L Manzel; D E Macfarlane

doi:10.1016/s0960-894x(99)00291-7

Structure-activity relationship analysis of substituted 4-quinolinamines, antagonists of immunostimulatory CpG-oligodeoxynucleotides

Bioorg Med Chem Lett. 1999 Jul 5;9(13):1819-24. doi: 10.1016/s0960-894x(99)00291-7.

Authors

L Strekowski¹, O Zegrocka, M Henary, M Say, M J Mokrosz, B M Kotecka, L Manzel, D E Macfarlane

Affiliation

¹ Department of Chemistry, Georgia State University, Atlanta 30303, USA.

PMID: 10406648
DOI: 10.1016/s0960-894x(99)00291-7

Abstract

On the basis of a systematic SAR analysis of substituted quinolines, a derivative 32 was synthesized that shows half-maximal inhibition of the immunostimulatory effect of CpG-oligodeoxynucleotides in vitro at the concentration of 0.24 nM.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Aminoquinolines / chemical synthesis*
Aminoquinolines / pharmacology*
Chloroquine / analogs & derivatives
CpG Islands / immunology
Kinetics
Oligonucleotides / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Aminoquinolines
Oligonucleotides
Chloroquine