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Journal of Bioactive and Compatible Polymers
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Mimicry of Biological Macromolecules by Polyaromatic Anionic Compounds

John R. Regan

Department of Medicinal Chemistry Rhône-Poulenc Rorer Central Research 500 Arcola Road Collegeville, PA 19426-0107

Joseph G. Bruno

Department of Medicinal Chemistry Rhône-Poulenc Rorer Central Research 500 Arcola Road Collegeville, PA 19426-0107

Mike N. Chang

Department of Medicinal Chemistry Rhône-Poulenc Rorer Central Research 500 Arcola Road Collegeville, PA 19426-0107

Ralph Sabatino

Department of Process Discovery Rhône-Poulenc Rorer Central Research 500 Arcola Road Collegeville, PA 19426-0107

Rose D'Alisa

Department of Process Discovery Rhône-Poulenc Rorer Central Research 500 Arcola Road Collegeville, PA 19426-0107

Shmuel A. Ben-Sasson

Department of Experimental Medicine and Cancer Research Hebrew University, Hadassah Medical School Ein Karem Jerusalem, Israel

Dan Eilat

Department of Medicine Hadassah University Hospital Ein Karem Jerusalem, Israel

The preparation, characterization and biological properties of some polyanionic polymers are reported. These polymers are constructed with repeating phenol-based monomers. The anionic groups attached to the aro matic nucleus provide the basis for binding to basic domains of proteins. Scaf fold flexibility permits the polyanionic polymers to adopt low energy conforma tions suitable for interacting with coagulation proteins and an anti-DNA monoclonal antibody. Structure activity relationships (SAR) and comparisons with aurintricarboxylic acid are described. The polymers doubled the clotting time in the APTT assay with value ranging from 10-1000 µg/mL. Binding to an anti-DNA monoclonal antibody occurred with ICso values of 0.3-5.0 µg/mL.

Journal of Bioactive and Compatible Polymers, Vol. 8, No. 4, 317-337 (1993)
DOI: 10.1177/088391159300800402
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