1
|
A mild and selective method for the hydrolysis of esters with trimethyltin hydroxide.
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Angew Chem Int Ed Engl
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2005
|
2.09
|
2
|
Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers.
|
Nature
|
2013
|
1.52
|
3
|
Total synthesis of thiostrepton. Retrosynthetic analysis and construction of key building blocks.
|
J Am Chem Soc
|
2005
|
1.30
|
4
|
Total synthesis of thiostrepton. Assembly of key building blocks and completion of the synthesis.
|
J Am Chem Soc
|
2005
|
1.26
|
5
|
Discovery of a biologically active thiostrepton fragment.
|
J Am Chem Soc
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2005
|
1.20
|
6
|
Identification of imidazo-pyrrolopyridines as novel and potent JAK1 inhibitors.
|
J Med Chem
|
2012
|
1.10
|
7
|
Universal solid-phase approach for the immobilization, derivatization, and resin-to-resin transfer reactions of boronic acids.
|
J Org Chem
|
2002
|
0.93
|
8
|
Total synthesis of thiostrepton, part 2: construction of the quinaldic acid macrocycle and final stages of the synthesis.
|
Angew Chem Int Ed Engl
|
2004
|
0.91
|
9
|
Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.
|
J Med Chem
|
2013
|
0.89
|
10
|
A biomimetically inspired synthesis of the dehydropiperidine domain of thiostrepton.
|
Angew Chem Int Ed Engl
|
2002
|
0.86
|
11
|
Structure-based identification of ureas as novel nicotinamide phosphoribosyltransferase (Nampt) inhibitors.
|
J Med Chem
|
2013
|
0.86
|
12
|
Total synthesis of thiostrepton, part 1: construction of the dehydropiperidine/thiazoline-containing macrocycle.
|
Angew Chem Int Ed Engl
|
2004
|
0.86
|
13
|
Preclinical disposition and pharmacokinetics-pharmacodynamic modeling of biomarker response and tumour growth inhibition in xenograft mouse models of G-573, a MEK inhibitor.
|
Xenobiotica
|
2010
|
0.84
|
14
|
Construction of substituted N-hydroxyindoles: synthesis of a nocathiacin I model system.
|
Angew Chem Int Ed Engl
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2005
|
0.83
|
15
|
A restricted role for TYK2 catalytic activity in human cytokine responses revealed by novel TYK2-selective inhibitors.
|
J Immunol
|
2013
|
0.83
|
16
|
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
|
Bioorg Med Chem Lett
|
2013
|
0.81
|
17
|
Fragment-based identification of amides derived from trans-2-(pyridin-3-yl)cyclopropanecarboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
|
J Med Chem
|
2014
|
0.81
|
18
|
Synthetic studies on thiostrepton: construction of thiostrepton analogues with the thiazoline-containing macrocycle.
|
Angew Chem Int Ed Engl
|
2003
|
0.80
|
19
|
Structural and biochemical analyses of the catalysis and potency impact of inhibitor phosphoribosylation by human nicotinamide phosphoribosyltransferase.
|
Chembiochem
|
2014
|
0.77
|
20
|
Discovery of potent and efficacious urea-containing nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with reduced CYP2C9 inhibition properties.
|
Bioorg Med Chem Lett
|
2013
|
0.77
|
21
|
Identification of 2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-derived ureas as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
|
Bioorg Med Chem Lett
|
2013
|
0.76
|
22
|
Design and evaluation of novel 8-oxo-pyridopyrimidine Jak1/2 inhibitors.
|
Bioorg Med Chem Lett
|
2013
|
0.76
|
23
|
Novel triazolo-pyrrolopyridines as inhibitors of Janus kinase 1.
|
Bioorg Med Chem Lett
|
2013
|
0.76
|
24
|
A probabilistic method to report predictions from a human liver microsomes stability QSAR model: a practical tool for drug discovery.
|
J Comput Aided Mol Des
|
2015
|
0.75
|
25
|
Stereocontrolled synthesis of the quinaldic acid macrocyclic system of thiostrepton.
|
Angew Chem Int Ed Engl
|
2002
|
0.75
|
26
|
Measuring NAD(+) levels in mouse blood and tissue samples via a surrogate matrix approach using LC-MS/MS.
|
Bioanalysis
|
2014
|
0.75
|
27
|
Structure-based discovery of C-2 substituted imidazo-pyrrolopyridine JAK1 inhibitors with improved selectivity over JAK2.
|
Bioorg Med Chem Lett
|
2012
|
0.75
|