Yusuf Hamied Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, UK.
Org Biomol Chem. 2022 Nov 23;20(45):8855-8858. doi: 10.1039/d2ob01819e.
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.
噻唑鎓环被其他环取代的硫胺素/TPP 类似物可有效抑制依赖硫胺素焦磷酸（TPP）的酶，但目前报道的类似物中心环的种类有限。我们报告了一种新型的类似物，吡哆醛，其中心环为吡咯环。我们进一步开发了吡哆醛衍生物作为丙酮酸脱氢酶的有效且选择性抑制剂，其可能具有抗癌潜力。
