68507-72-2Relevant academic research and scientific papers
Cathepsin B inhibitors: Further exploration of the nitroxoline core
Sosi?, Izidor,Mitrovi?, Ana,?uri?, Hrvoje,Knez, Damijan,Brodnik ?ugelj, Helena,?tefane, Bogdan,Kos, Janko,Gobec, Stanislav
supporting information, p. 1239 - 1247 (2018/03/05)
Human cathepsin B is a cysteine protease with many house-keeping functions, such as intracellular proteolysis within lysosomes. Its increased activity and expression have been strongly associated with many pathological processes, including cancers. We present here the design and synthesis of novel derivatives of nitroxoline as inhibitors of cathepsin B. These were prepared either by omitting the pyridine part, or by modifying positions 2, 7, and 8 of nitroxoline. All compounds were evaluated for their ability to inhibit endopeptidase and exopeptidase activities of cathepsin B. For the most promising inhibitors, the ability to reduce extracellular and intracellular collagen IV degradation was determined, followed by their evaluation in cell-based in vitro models of tumor invasion. The presented data show that we have further defined the structural requirements for cathepsin B inhibition by nitroxoline derivatives and provided additional knowledge that could lead to non-peptidic compounds with usefulness against tumor progression.
Synthesis of functionalized carbamates and quinones via sequential oxidation of salicylaldehydes using TBHP as the oxidant
Rajendra Prasad,Suresh,Ravikumar,Reddy, N. Veera,Reddy, K. Rajender
supporting information, p. 6307 - 6310 (2014/12/10)
A sequential oxidative approach was designed to functionalize salicylaldehyde derivatives and provide corresponding bi-functional amide-carbamate and amide-quinone units. A combination of metal/metal free conditions and TBHP as the external oxidant provid
