Synthesis of pyrrothiamine, a novel thiamine analogue, and evaluation of derivatives as potent and selective inhibitors of pyruvate dehydrogenase

Autor: Alex H. Y. Chan, Terence C. S. Ho, Kwasi Agyei-Owusu, Finian J. Leeper
Přispěvatelé: Leeper, Finian [0000-0003-3408-5199], Apollo - University of Cambridge Repository
Rok vydání: 2022
Předmět:
Zdroj: Organicbiomolecular chemistry. 20(45)
ISSN: 1477-0539
Popis: Inhibition of thiamine pyrophosphate (TPP)-dependent enzymes with thiamine/TPP analogues that have the central thiazolium ring replaced with other rings is well established, but a limited number of central rings have been reported. We report a novel analogue, pyrrothiamine, with a central pyrrole ring. We further develop pyrrothiamine derivatives as potent and selective inhibitors of pyruvate dehydrogenase, which might have anti-cancer potential.
Databáze: OpenAIRE