Quevedo, Camilo E.; Bataille, Carole J. R.; Byrne, Simon; Durbin, Matthew; Elkins, Jon; Guillermo, Abigail; Jones, Alan M.; Knapp, Stefan; Nadali, Anna; Walker, Roderick G.; Wilkinson, Isabel V. L.; Wynne, Graham M.; Davies, Stephen G.; Russell, Angela J. published the artcile< Aminothiazolones as potent, selective and cell active inhibitors of the PIM kinase family>, Computed Properties of 45434-02-4, the main research area is aminothiazolone drug discovery synthesis anticancer agent PIM kinase inhibitor.
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 optimization of those compounds to improve their physicochem. and ADME properties as well as reducing their off-targets activities against other kinases. Through mol. modeling and systematic structure activity relationship (SAR) studies, advanced mols. with high inhibitory potency, reduced off-target activity and minimal efflux were identified as new pan-PIM inhibitors. One example of an early lead, I, was found to inhibit PIMs with nanomolar potency (15 nM for PIM1), inhibit proliferation of two PIM-expressing leukemic cancer cell lines, MV4-11 and K562, and to reduce intracellular phosphorylation of a PIM substrate in a concentration dependent manner.
Bioorganic & Medicinal Chemistry published new progress about Antitumor agents. 45434-02-4 belongs to class alcohols-buliding-blocks, and the molecular formula is C5H11NO, Computed Properties of 45434-02-4.
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