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- W3080973670 abstract "Abstract We have previously reported the discovery of a series of rhodanine-based inhibitors of the PIM family of serine/threonine kinases. Here we described the optimisation of those compounds to improve their physicochemical and ADME properties as well as reducing their off-targets activities against other kinases. Through molecular modeling and systematic structure activity relationship (SAR) studies, advanced molecules with high inhibitory potency, reduced off-target activity and minimal efflux were identified as new pan-PIM inhibitors. One example of an early lead, OX01401, was found to inhibit PIMs with nanomolar potency (15 nM for PIM1), inhibit proliferation of two PIM-expressing leukaemic cancer cell lines, MV4-11 and K562, and to reduce intracellular phosphorylation of a PIM substrate in a concentration dependent manner." @default.
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- W3080973670 date "2020-11-01" @default.
- W3080973670 modified "2023-10-17" @default.
- W3080973670 title "Aminothiazolones as potent, selective and cell active inhibitors of the PIM kinase family" @default.
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- W3080973670 doi "https://doi.org/10.1016/j.bmc.2020.115724" @default.
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