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Structure-Guided Evolution of Potent and Selective CHK1 Inhibitors through Scaffold Morphing
The optimization of the pyrazolopyridines to a series of potent andCHK1-selective isoquinolines demonstrates how fragment-growing and scaffold morphing strategies arising from a structure-based understanding of CHK1 inhibitor binding can be combined to successfully progress fragment-derived hit matter to compounds with activity in vivo.
Cell penetrable peptoid carrier vehicles: synthesis and evaluation.
Using a highly efficient solid-phase route a series of fluorescein conjugated peptoid oligomers were synthesised and observed to display remarkable cell penetrating properties, offering the
L‐Arginyl‐3,4‐Spermidine is neuroprotective in several in vitro models of neurodegeneration and in vivo ischaemia without suppressing synaptic transmission
It is demonstrated that L‐Arg‐3,4 is protective in several models of neurodegeneration and may have potential as a new therapeutic compound for the treatment of stroke, trauma, and other neurodegnerative diseases.
Protecting groups in solid-phase organic synthesis.
Thiophene-S,S-dioxidized indophenine (IDTO) based donor–acceptor polymers for n-channel organic thin film transistors
Two donor–acceptor (D–A) conjugated polymers, PIDTOBT and PIDTOBTz, based on thiophene-S,S-dioxidized indophenine (IDTO) as the acceptor building block are synthesized for solution processed organic