30652-22-3Relevant articles and documents
Synthesis, Modification, and Biological Evaluation of a Library of Novel Water-Soluble Thiopyridone-Based Organometallic Complexes and Their Unexpected (Biological) Behavior
Gajic, Natalie,Happl, Barbara,Harringer, Sophia,Hejl, Michaela,Jakupec, Michael A.,Kandioller, Wolfgang,Kast, Caroline,Keppler, Bernhard K.,Koellensperger, Gunda,Legin, Anton A.,Ozenil, Marius,Roller, Alexander,Schweikert, Andreas,Wernitznig, Debora
supporting information, (2020/04/20)
A series of 16 dinuclear thiopyridone-based organometallics with excellent water solubility, increased stability and remarkable cytotoxicity were synthesized and characterized. The complexes of this work formed dimeric species featuring a double positive charge in polar protic solvents, accounting for their outstanding solubility in aqueous solution. Most of them displayed higher antiproliferative activity than their parental thiomaltol complex, with unexpected cytotoxicity trends depending on the employed metal center, ligand modification, and cell line. Insights into their behavior in biological systems were gathered by means of amino-acid interaction studies, cytotoxicity tests in 3D spheroid models, laser ablation, cellular accumulation measurements, as well as cell cycle experiments.
Synthesis, molecular modelling and biological studies of 3-hydroxy-pyrane-4-one and 3-hydroxy-pyridine-4-one derivatives as HIV-1 integrase inhibitors
Sirous, Hajar,Fassihi, Afshin,Brogi, Simone,Campiani, Giuseppe,Christ, Frauke,Debyser, Zeger,Gemma, Sandra,Butini, Stefania,Chemi, Giulia,Grillo, Alessandro,Zabihollahi, Rezvan,Aghasadeghi, Mohammad R.,Saghaie, Lotfollah,Memarian, Hamid R.
, p. 755 - 770 (2019/11/02)
Background: Despite the progress in the discovery of antiretroviral compounds for treating HIV-1 infection by targeting HIV integrase (IN), a promising and well-known drug target against HIV-1, there is a growing need to increase the armamentarium against
4-Pyridone derivatives as new inhibitors of bacterial enoyl-ACP reductase FabI
Kitagawa, Hideo,Kumura, Ko,Takahata, Sho,Iida, Maiko,Atsumi, Kunio
, p. 1106 - 1116 (2008/02/01)
Bacterial FAS provides essential fatty acids for use in the assembly of key cellular components. Among them, FabI is an enoyl-ACP reductase which catalyzes the final and rate-limiting step of bacterial FAS. It is a potential target for selective antibacterial action, because it shows low overall sequence homology with mammalian enzymes. Until today, various compounds have been reported as inhibitors of bacterial FabI-inhibitory compounds. To discover novel small-molecular FabI inhibitors, we initially screened our compound library for inhibitory activity toward FabI of Escherichia coli. And discovered 4-pyridone derivatives as a lead compound. Structure optimization studies yielded 4-pyridone derivatives 7n having strong FabI-inhibitory and antibacterial activities against Staphylococcus aureus. There have been no reports concerning 4-pyridone derivatives as FabI inhibitor.