Boronic ester derivative-dependent activity of parthenolide analogues

28 October 2021, Version 2
This content is a preprint and has not undergone peer review at the time of posting.

Abstract

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.

Keywords

Parthenolide
Prodrug
boron
boronic ester
Hydrolysis
ROS
Oxidation
logP
Drug-like
CLL
Leukaemia
Leukemia
Chronic lymphocytic leukemia
pro-oxidant

Supplementary materials

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Description
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Title
Supplementary Material
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Supplementary Material: Boronic ester derivative-dependent activity of parthenolide analogues
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