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

Published version
Peer-reviewed

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Authors

Leeper, Finian J 
Chan, Alex HY 
Ho, Terence CS 
Agyei-Owusu, Kwasi 

Abstract

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.

Description

Keywords

Thiamine, Thiamine Pyrophosphate, Diphosphates, Oxidoreductases, Pyruvates, Pyruvate Dehydrogenase Complex

Journal Title

Organic and Biomolecular Chemistry

Conference Name

Journal ISSN

1477-0520
1477-0539

Volume Title

Publisher

Royal Society of Chemistry
Sponsorship
K.M. Medhealth