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Boronic ester derivative-dependent activity of parthenolide analogues

28 October 2021, Version 1
Working Paper
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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Supplementary Material
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Supplementary Material: Boronic ester derivative-dependent activity of parthenolide analogues
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Version History

Oct 28, 2021 Version 1

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The content is available under CC BY NC ND 4.0 [opens in a new tab]

DOI

10.26434/chemrxiv-2021-hzfk2
D O I: 10.26434/chemrxiv-2021-hzfk2 [opens in a new tab]

Funding

University of Birmingham
EPSRC
EP/K039245/1
EPSRC
Internally allocated: ISF 2012
MRC
Internally allocated: Confidence in Concepts 14/15
Bloodwise
14031
CRUK
C20807/A2864
The Royal Society
International Exchange Grant
Welch Regents Chair
F-0046
University of Manchester

Author’s competing interest statement

The author(s) have declared they have no conflict of interest with regard to this content

Ethics

The author(s) have declared ethics committee/IRB approval is not relevant to this content

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