TY - UNPB
T1 - Boronic ester derivative-dependent activity of parthenolide analogues
AU - Li, Xingjian
AU - Williams, George
AU - Quy, Alex
AU - Zhao, Yiming
AU - Male, Louise
AU - Anslyn, Eric
AU - Stankovic, Tatjana
AU - Leach, Andrew
AU - Agathanggelou, Angelo
AU - Fossey, John
PY - 2021/10/28
Y1 - 2021/10/28
N2 - 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.
AB - 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.
U2 - 10.33774/chemrxiv-2021-hzfk2
DO - 10.33774/chemrxiv-2021-hzfk2
M3 - Preprint
BT - Boronic ester derivative-dependent activity of parthenolide analogues
PB - ChemRxiv
ER -