Novel fluorinated acridone derivatives. Part 1: Synthesis and evaluation as potential anticancer agents

• Published in: Bioorganic & medicinal chemistry letters 2008-07, Vol.18 (14), p.4172-4176
• Main Authors: Fadeyi, Olugbeminiyi O., Adamson, Saudat T., Myles, E. Lewis, Okoro, Cosmas O.
• Format: Article
• Language: English
• Subjects: Acridine; Acridines - chemical synthesis; Acridines - chemistry; Acridone; Acridones; Anticancer; Antineoplastic agents; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - pharmacology; Biological and medical sciences; Cell Line, Tumor; Chemistry, Pharmaceutical - methods; DNA; DNA - chemistry; Drug Design; Drug Screening Assays, Antitumor; Fluorinated; Fluorine - chemistry; General aspects; Humans; Inhibitory Concentration 50; Medical sciences; Models, Chemical; Pharmacology. Drug treatments; Structure-Activity Relationship; Time Factors; Tricyclic
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2008.05.078

We report on the synthesis of a novel series of fluorinated acridones from 5-trifluoromethyl-1,3-cyclohexanedione. The cytotoxic activities of the compounds were studied in several cancer cells. Compounds 9a, 9c, 9e, 9f, and 9h exhibited significant anticancer activities in selected cell lines. Compound 9c is the most active showing GI 50 that ranged in values from 0.13 to 26 μM, covering a wide range of cancer cell lines. We report on the synthesis of a novel series of fluorinated acridones from 5-trifluoromethyl-1,3-cyclohexanedione. The cytotoxic activities of the compounds were studied in several cancer cells. Compounds 9a, 9c, 9e, 9f, and 9h exhibited significant anticancer activities in selected cell lines. Compound 9c is the most active showing GI 50 that ranged in values from 0.13 to 26 μM, covering a wide range of cancer cell lines.