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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.
- I. Peretto, R. Sánchez-Martín, Xui-hong Wang, J. Ellard, S. Mittoo, M. Bradley
- Chemistry, BiologyChemical communications
- 2 September 2003
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…
Design and evaluation of 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines as inhibitors of checkpoint and other kinases.
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.
Efficient room temperature copper(I) mediated 5-endo radical cyclisations
Synthesis of the C9C25 fragment of L-755,807. Evidence for the relative configuration of the side-chain
Fluorescence enhancement through enzymatic cleavage of internally quenched dendritic peptides: a sensitive assay for the AspN endoproteinase.
Identification and optimisation of a series of tetrahydrobenzotriazoles as metabotropic glutamate receptor 5-selective positive allosteric modulators that improve performance in a preclinical model…
Thiophene-S,S-dioxidized indophenine (IDTO) based donor–acceptor polymers for n-channel organic thin film transistors
- Yunfeng Deng, Jesse Quinn, Bin Sun, Yinghui He, J. Ellard, Yuning Li
- Chemistry, Materials Science
- 6 April 2016
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…