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2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines.
TLDR
2-Anilino-4-(benzimidazol-2-yl)-pyrimidines were shown to inhibit four cancer-related protein kinases and exhibited antiproliferative activity for several cancer cell lines of the NCI in vitro cell line panel in submicromolar concentrations.
9- and 11-Substituted 4-azapaullones are potent and selective inhibitors of African trypanosoma.
TLDR
4-azapaullones carrying α,β-unsaturated carbonyl chains in 9- or 11-position were synthesized employing a procedure with a Heck reaction as key step and proved to be potent antiparasitic agents with antitrypanosomal activity in the submicromolar range.
3,6-Diamino-4-(2-halophenyl)-2-benzoylthieno[2,3-b]pyridine-5-carbonitriles are selective inhibitors of Plasmodium falciparum glycogen synthase kinase-3.
TLDR
It was found that subtle differences in the ATP-binding pockets are responsible for the observed PfGSk-3 vs HsGSK-3 selectivity, and suggest that inhibitors of PfGSK -3 could be developed as potential antimalarial drugs.
10-Iodo-11H-indolo[3,2-c]quinoline-6-carboxylic Acids Are Selective Inhibitors of DYRK1A
TLDR
Structural modification of the screening hit 11H-indolo[3,2-c]quinoline-6-carboxylic acid revealed structure–activity relationships for kinase inhibition and enabled the design of 10-iodo-substituted derivatives as very potent DYRK1A inhibitors with considerable selectivity against CLKs.
Identification of 2-anilino-9-methoxy-5,7-dihydro-6H-pyrimido[5,4-d][1]benzazepin-6-ones as dual PLK1/VEGF-R2 kinase inhibitor chemotypes by structure-based lead generation.
To develop multikinase inhibitors with dual PLK1/VEGF-R2 inhibitory activity, the d-annulated 1-benzazepin-2-one scaffold present in the paullone family of kinase inhibitors was investigated as a
2-Arylpaullones are selective antitrypanosomal agents.
TLDR
The most potent compound identified in this study was 9-tert-butyl-2-(4-morpholinophenyl)paullone (3i) which inhibited the parasites at submicromolar concentrations (GI50 = 510 nM) with a selectivity index of 157.
Evaluation of monolithic HPLC columns for various pharmaceutical separations: method transfer from conventional phases and batch to batch repeatability.
Methods developed on conventional particle-packed C18 columns for pilocarpine, propranolol, glibenclamide, glimepiride, insulin and their respective degradation products or related compounds were
Inhibitors of the RET tyrosine kinase based on a 2-(alkylsulfanyl)-4-(3-thienyl)nicotinonitrile scaffold.
TLDR
Docking experiments suggest a binding mode of the new inhibitors in the ATP binding pocket of the target kinase, explaining the observed structure-activity relationships.
Wide concentration range investigation of recovery, precision and error structure in liquid chromatography.
TLDR
It is concluded that with the injection error being constant the peak integration error becomes the dominating error source at low concentrations, e.g. at concentrations below the five-fold of the LOQ.
Precise, fast, and flexible determination of protein interactions by affinity capillary electrophoresis: Part 3: Anions
TLDR
ACE has been applied here for comprehensively studying the influence of various anions on proteins of BSA, β‐lactoglobulin, ovalbumin, myoglobin, and lysozyme and circular dichroism has been used as an orthogonal approach to characterize the interactions between the studied proteins and anions to confirm the ACE results.
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