Boronic ester derivative-dependent activity of parthenolide analogues

Xingjian Li, George Williams, Alex Quy, Yiming Zhao, Louise Male, Eric Anslyn, Tatjana Stankovic, Andrew Leach, Angelo Agathanggelou, John Fossey

Research output: Working paper/PreprintPreprint


Four parthenolide derived prodrugs, containing different boronic ester moieties, were synthesised, their drug-like properties were calculated and their activity against chronic lymphocytic leukaemia (CLL) MEC1 cells measured. Differences in the clogP, the propensity towards oxidation by hydrogen peroxide, the affinity of the associated diols to a model boronic acid and the biological activity against MEC1 cells were contrasted, and it was found that the propensity for oxidation correlated to biological activity.
Original languageEnglish
Publication statusPublished - 28 Oct 2021


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