| Autor: |
Nicolas Boutard, Arkadiusz Białas, Aleksandra Sabiniarz, Paweł Guzik, Katarzyna Banaszak, Artur Biela, Marcin Bień, Anna Buda, Barbara Bugaj, Ewelina Cieluch, Anna Cierpich, Łukasz Dudek, Hans-Michael Eggenweiler, Joanna Fogt, Monika Gaik, Andrzej Gondela, Krzysztof Jakubiec, Mirek Jurzak, Agata Kitlińska, Piotr Kowalczyk, Maciej Kujawa, Katarzyna Kwiecińska, Marcin Leś, Ralph Lindemann, Monika Maciuszek, Maciej Mikulski, Paulina Niedziejko, Alicja Obara, Henryk Pawlik, Tomasz Rzymski, Magdalena Sieprawska-Lupa, Marta Sowińska, Joanna Szeremeta-Spisak, Agata Stachowicz, Mateusz M. Tomczyk, Katarzyna Wiklik, Łukasz Włoszczak, Sylwia Ziemiańska, Adrian Zarębski, Krzysztof Brzózka, Mateusz Nowak, Charles-Henry Fabritius |
| Jazyk: |
angličtina |
| Rok vydání: |
2019 |
| Předmět: |
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| Popis: |
In oncology, the "Warburg effect" describes the elevated production of energy by glycolysis in cancer cells. The ubiquitous and hypoxia-induced 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3) plays a noteworthy role in the regulation of glycolysis by producing fructose-2,6-biphosphate (F-2,6-BP), a potent activator of the glycolysis rate-limiting phosphofructokinase PFK-1. Series of amides and sulfonamides derivatives based on a N-aryl 6-aminoquinoxaline scaffold were synthesized and tested for their inhibition of PFKFB3 in vitro in a biochemical assay as well as in HCT116 cells. The carboxamide series displayed satisfactory kinetic solubility and metabolic stability, and within this class, potent lead compounds with low nanomolar activity have been identified with a suitable profile for further in vivo evaluation. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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