55557-48-7Relevant academic research and scientific papers
GLUCOSE UPTAKE INHIBITORS AND USES THEREOF
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Paragraph 00487, (2021/05/21)
The present invention relates to novel compounds that modulate cellular glucose uptake by affecting various targets, including, but not limited to those related to glycolysis and known transporters/co-transporters of the GLUT family. The compounds according to the invention are useful for treating cancer such as: neuroendrocrine neoplasms, gastrointestinal stromal tumors (GIST), renal cell carcinoma, paraganglioma, pheochromocytoma, pituitary adenoma, colorectal cancer, lung cancer, gastric cancer, pancreatic cancer sarcoma, head and neck cancer, melanoma, ovarian cancer and other cancers that rely on high levels of glycolysis for survival and proliferation; as well as in treating of autoimmune diseases, inflammation, infectious diseases, and metabolic diseases.
Synthesis and characterization of 1,2,4-triazolo[1,5-a]pyrimidine-2-carboxamide-based compounds targeting the PA-PB1 interface of influenza A virus polymerase
Massari, Serena,Bertagnin, Chiara,Pismataro, Maria Chiara,Donnadio, Anna,Nannetti, Giulio,Felicetti, Tommaso,Di Bona, Stefano,Nizi, Maria Giulia,Tensi, Leonardo,Manfroni, Giuseppe,Loza, Maria Isabel,Sabatini, Stefano,Cecchetti, Violetta,Brea, Jose,Goracci, Laura,Loregian, Arianna,Tabarrini, Oriana
, (2020/10/27)
Influenza viruses (Flu) are responsible for seasonal epidemics causing high rates of morbidity, which can dramatically increase during severe pandemic outbreaks. Antiviral drugs are an indispensable weapon to treat infected people and reduce the impact on
INHIBITORS OF MICROBIAL BETA-GLUCURONIDASE ENZYMES AND USES THEREOF
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Page/Page column 58, (2018/02/28)
Compounds and compositions are provided that comprise selective b-glucuronidase inhibitors. The compounds and compositions can ameliorate the side effects of chemotherapeutic agents and can improve the efficacy of such agents, including irinotecan and non-steroidal anti-inflammatory drugs.
INHIBITORS OF MICROBIAL BETA-GLUCURONIDASE ENZYMES AND USES THEREOF
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Page/Page column 67, (2018/08/26)
Methods utilizing compounds and compositions are provided that comprise selective β-glucuronidase inhibitors. The methods can ameliorate the side effects of chemotherapeutic agents and can improve the efficacy of such agents, including irinotecan and non-steroidal anti-inflammatory drugs. The methods comprise administering the compounds in combination with agents or administering the compounds in a monotherapy for the treatment of cancer and gastrointestinal conditions.
Synthesis and evaluation of pyrido-thieno-pyrimidines as potent and selective Cdc7 kinase inhibitors
Zhao, Chunlin,Tovar, Christian,Yin, Xuefeng,Xu, Qui,Todorov, Ivan T.,Vassilev, Lyubomir T.,Chen, Li
scheme or table, p. 319 - 323 (2011/02/26)
Cdc7 kinase plays a critical role in the regulation of DNA replication in eukaryotic cells and has been proposed as a target for cancer therapy. We have identified a class of Cdc7/Dbf4 inhibitors with a pyrido-thieno-pyrimidine core structure. Synthesis o
Evolution of the thienopyridine class of inhibitors of IκB kinase-β: Part I: Hit-to-lead strategies
Morwick, Tina,Berry, Angela,Brickwood, Janice,Cardozo, Mario,Catron, Katrina,DeTuri, Molly,Emeigh, Jonathan,Homon, Carol,Hrapchak, Matt,Jacober, Stephen,Jakes, Scott,Kaplita, Paul,Kelly, Terence A.,Ksiazek, John,Liuzzi, Michel,Magolda, Ronald,Mao, Can,Marshall, Daniel,McNeil, Daniel,Prokopowicz II, Anthony,Sarko, Christopher,Scouten, Erika,Sledziona, Cynthia,Sun, Sanxing,Watrous, Jane,Wu, Jiang Ping,Cywin, Charles L.
, p. 2898 - 2908 (2007/10/03)
High-throughput screening is routinely employed as a method for the identification of novel hit structures. Large numbers of active compounds are typically procured in this way and must undergo a rigorous validation process. This process is described in detail for a collection of screening hits identified as inhibitors of IκB kinase-β (IKKβ), a key regulatory enzyme in the nuclear factor-κB (NF-κB) pathway. From these studies, a promising hit series was selected. Subsequent lead generation activities included the development of a pharmacophore hypothesis and structure-activity relationship (SAR) for the hit series. This led to the exploration of related scaffolds offering additional opportunities, and the various structural classes were comparatively evaluated for enzyme inhibition, selectivity, and drug-like properties. A novel lead series of thienopyridines was thereby established, and this series advanced into lead optimization for further development.
Nucleophilic Displacements in Pyridine Rings
Dunn, A. D.,Norrie, R.
, p. 85 - 89 (2007/10/02)
The reactions of halopyridines containing an electron withdrawing group (-CN, -CO2R, -COMe, -NO2) with sulphur nucleophiles is reported.
