Synthesis and cytostatic activity of 4,7-dihydroxythioaurone derivatives. Effect of B ring substitution on the activity.
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.
Konieczny
Marek Tadeusz
MT
Department of Organic Chemistry, Medical University of Gdańsk, Poland. markon@amg.gda.pl
Konieczny
Wojciech
W
Okabe
Soko
S
Tsujimoto
Hiroaki
H
Suda
Yoshimitsu
Y
Wierzba
Konstanty
K
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006574:Heterocyclic Compounds, 2-Ring / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis* / Q000494:pharmacology*
D000970:Antineoplastic Agents; D006574:Heterocyclic Compounds, 2-Ring; D013876:Thiophenes