Synthesis and Cytostatic Activity of 4,7-Dihydroxythioaurone Derivatives. Effect of B Ring Substitution on the Activity

• Published in: Chemical & Pharmaceutical Bulletin Vol. 54; no. 3; pp. 350 - 353
• Main Authors: Konieczny, Marek Tadeusz, Konieczny, Wojciech, Okabe, Soko, Tsujimoto, Hiroaki, Suda, Yoshimitsu, Wierzba, Konstanty
• Format: Journal Article
• Language: English
• Published: TOKYO The Pharmaceutical Society of Japan 01.03.2006; Pharmaceutical Society of Japan; Pharmaceutical Soc Japan; Japan Science and Technology Agency
• Subjects: Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - pharmacology; antitumor; Cell Line, Tumor; Chemistry; Chemistry, Medicinal; Chemistry, Multidisciplinary; cytotoxicity; Drug Screening Assays, Antitumor; Heterocyclic Compounds, 2-Ring - chemistry; Heterocyclic Compounds, 2-Ring - pharmacology; Humans; Life Sciences & Biomedicine; Magnetic Resonance Spectroscopy; Pharmacology & Pharmacy; Physical Sciences; Science & Technology; Structure-Activity Relationship; thioaurone; Thiophenes - chemical synthesis; Thiophenes - pharmacology; FLAVONOIDS; antitumor; thioaurone; cytotoxicity
• ISSN: 0009-2363; 1347-5223
• DOI: 10.1248/cpb.54.350

Biological activity of thioaurones was not tested so far and the group constitute completely unexplored source of new molecules of pharmacological interest. We report synthesis and evaluation of cytotoxic activity of thioaurone derivatives bearing p-hydroquinone system in ring A. Their activity was found to depend strongly on substitution pattern, so eventually both the activity and pharmacokinetic parameters of the molecules could be tailored by further structural modifications.