Aryl rings are part of the darpone pharmacophore.
In order to investigate structure-activity relationships in the antiproliferative darpone series, the derivatives 8a and 8b lacking the aryl substituents in either 2- or 4-position were synthesized and evaluated for cancer cell growth inhibition. Since both 8a and 8b were devoid of noteworthy antiproliferative activity, both aryl substituents can be considered as part of the darpone pharmacophore.
Schultz
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Universität Hamburg, Institut für Pharmazie, Bundesstrasse 45, D-20146 Hamburg, Germany.
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Kunick
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D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001552:Benzazepines / Q000138:chemical synthesis* / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008826:Microbial Sensitivity Tests; D011084:Polycyclic Aromatic Hydrocarbons / Q000737:chemistry / Q000494:pharmacology; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured / Q000187:drug effects
D000970:Antineoplastic Agents; D001552:Benzazepines; D011084:Polycyclic Aromatic Hydrocarbons; D011725:Pyridines