125686-91-1Relevant academic research and scientific papers
Coordination chemistry and biological activity of 5′-OH modified quinoline-B12 derivatives
Zelenka, Karel,Brandl, Helmut,Spingler, Bernhard,Zelder, Felix
, p. 9665 - 9667 (2011)
The consequences of structural modifications at the 5′-OH ribofuranotide moiety of quinoline modified B12 derivatives are discussed in regard of the coordination chemistry, the electrochemical properties and the biological behaviour of the compound.
Design and Synthesis of 3-Carbamoylbenzoic Acid Derivatives as Inhibitors of Human Apurinic/Apyrimidinic Endonuclease 1 (APE1)
Aiello, Francesca,Shabaik, Yumna,Esqueda, Adrian,Sanchez, Tino W.,Grande, Fedora,Garofalo, Antonio,Neamati, Nouri
, p. 1825 - 1839 (2012/10/30)
Apurinic/apyrimidinic (AP) endonuclease 1 (APE1) is a multifaceted protein with an essential role in the base excision repair (BER) pathway. Its implication in tumor development, progression, and resistance has been confirmed in multiple cancers, making it a viable target for intensive investigation. In this work, we designed and synthesized different classes of small-molecule inhibitors of the catalytic endonuclease function of APE1 that contain a 3-carbamoylbenzoic acid scaffold. Further structural modifications were made with the aim of increasing the activity and cytotoxicity of these inhibitors. Several of our compounds were shown to inhibit the catalytic endonuclease function of APE1 with potencies in the low-micromolar range invitro, and therefore represent novel classes of APE1 inhibitors worthy of further development.
Synthesis and anti-inflammatory structure-activity relationships of thiazine-quinoline-quinones: Inhibitors of the neutrophil respiratory burst in a model of acute gouty arthritis
Chia, Elizabeth W.,Pearce, A. Norrie,Berridge, Michael V.,Larsen, Lesley,Perry, Nigel B.,Sansom, Catherine E.,Godfrey, Colette A.,Hanton, Lyall R.,Lu, Guo-Liang (Leon),Walton, Michaela,Denny, William A.,Webb, Victoria L.,Copp, Brent R.,Harper, Jacquie L.
experimental part, p. 9432 - 9442 (2009/04/11)
Sixteen new thiazine-quinoline-quinones have been synthesised, plus one bicyclic analogue. These compounds inhibited neutrophil superoxide production in vitro with IC50s as low 60 nM. Compounds with high in vitro anti-inflammatory activity were also tested in a mouse model of acute inflammation. The most active compounds inhibited both neutrophil infiltration and superoxide production at doses 2.5 μmol/kg, highlighting their potential for development as novel NSAIDs.
