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

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. On the basis of a systematic SAR analysis of substituted quin...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1999-07, Vol.9 (13), p.1819-1824
Hauptverfasser:	Strekowski, Lucjan, Zegrocka, Oliwia, Henary, Maged, Say, Martial, Mokrosz, Maria J., Kotecka, Barbara M., Manzel, Lori, Macfarlane, Donald E.
Format:	Artikel
Sprache:	eng
Schlagworte:	Aminoquinolines - chemical synthesis Aminoquinolines - pharmacology Biological and medical sciences Chloroquine - analogs & derivatives CpG Islands - immunology Immunomodulators Kinetics Medical sciences Oligonucleotides - antagonists & inhibitors Pharmacology. Drug treatments Structure-Activity Relationship
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Zusammenfassung:	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. On the basis of a systematic SAR analysis of substituted quinolines the powerful antagonist 32 (EC 50 = 0.24 nM) was synthesized.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(99)00291-7