Teuscher, Kevin B. published the artcileDiscovery of Potent Orally Bioavailable WD Repeat Domain 5 (WDR5) Inhibitors Using a Pharmacophore-Based Optimization, Name: (S)-2-Methylpropane-2-sulfinamide, the main research area is cancers WDR5 WIN site inhibitor selectivity pharmacokinetic antiproliferative bioavailability.
WD repeat domain 5 (WDR5) is a nuclear scaffolding protein that forms many biol. important multiprotein complexes. The WIN site of WDR5 represents a promising pharmacol. target in a variety of human cancers. Here, we describe the optimization of our initial WDR5 WIN-site inhibitor using a structure-guided pharmacophore-based convergent strategy to improve its druglike properties and pharmacokinetic profile. The core of the previous lead remained constant while a focused SAR effort on the three pharmacophore units was combined to generate a new in vivo lead series. Importantly, this new series of compounds has picomolar binding affinity, improved cellular antiproliferative activity and selectivity, and increased kinetic aqueous solubility They also exhibit a desirable oral pharmacokinetic profile with manageable i.v. clearance and high oral bioavailability. Thus, these new leads including compound 41 (I), are useful probes toward studying the effects of WDR5 inhibition.
Journal of Medicinal Chemistry published new progress about Acute myeloid leukemia. 343338-28-3 belongs to class amides-buliding-blocks, name is (S)-2-Methylpropane-2-sulfinamide, and the molecular formula is C4H11NOS, Name: (S)-2-Methylpropane-2-sulfinamide.
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