Novel fluorinated pseudopeptides as proteasome inhibitors.

Incorporation of fluorinated phenylalanine generates highly specific inhibitor of proteasome's chymotrypsin-like sites. J Med Chem (2010) 0.85

Oxadiazole-isopropylamides as potent and noncovalent proteasome inhibitors. J Med Chem (2013) 0.77

Interplay between Structure and Charge as a Key to Allosteric Modulation of Human 20S Proteasome by the Basic Fragment of HIV-1 Tat Protein. PLoS One (2015) 0.75

Novel synthesis of pseudopeptides bearing a difluoromethyl group by Ugi reaction and desulfanylation. Beilstein J Org Chem (2011) 0.75

Inhibition of human and yeast 20S proteasome by analogues of trypsin inhibitor SFTI-1. PLoS One (2014) 0.75

Defective ribosome assembly in Shwachman-Diamond syndrome. Blood (2011) 1.97

Uncoupling of GTP hydrolysis from eIF6 release on the ribosome causes Shwachman-Diamond syndrome. Genes Dev (2011) 1.89

Caspase-dependent protein phosphatase 2A activation contributes to endotoxin-induced cardiomyocyte contractile dysfunction. Crit Care Med (2010) 1.43

Transport of fluoroalkyl dihydroartemisinin derivatives across rat intestinal tissue. J Pharm Pharmacol (2008) 1.40

Analyses of the factors for the demagnetization of permanent magnets caused by high-energy electron irradiation. J Synchrotron Radiat (2009) 1.06

Towards the control of intracellular protein turnover: mitochondrial Lon protease inhibitors versus proteasome inhibitors. Biochimie (2007) 1.06

Design, synthesis and antimalarial activity of trifluoromethylartemisinin-mefloquine dual molecules. Chembiochem (2005) 1.03

Fluoroartemisinins: metabolically more stable antimalarial artemisinin derivatives. ChemMedChem (2007) 1.02

HIV-1 protease and reverse transcriptase control the architecture of their nucleocapsid partner. PLoS One (2007) 0.97

Non Lewis acid catalysed epoxide ring opening with amino acid esters. Org Biomol Chem (2009) 0.94

The chemistry of trifluoromethyl imines and related acetals derived from fluoral. Chem Soc Rev (2005) 0.92

Solvent-promoted and -controlled aza-Michael reaction with aromatic amines. J Org Chem (2009) 0.91

Disruption of the HIV-1 protease dimer with interface peptides: structural studies using NMR spectroscopy combined with [2-(13)C]-Trp selective labeling. Biopolymers (2007) 0.91

Mutational analysis of the CG recognizing DNA methyltransferase SssI: insight into enzyme-DNA interactions. Biochim Biophys Acta (2009) 0.90

Coumarinic derivatives show anti-inflammatory effects on alveolar macrophages, but their anti-elastase activity is essential to reduce lung inflammation in vivo. Int Immunopharmacol (2008) 0.90

Stabilization of mutant p53 via alkylation of cysteines and effects on DNA binding. Protein Sci (2010) 0.90

Cholestasis is associated with hepatic microvascular dysfunction and aberrant energy metabolism before and during ischemia-reperfusion. Antioxid Redox Signal (2012) 0.86

Dimer disruption and monomer sequestration by alkyl tripeptides are successful strategies for inhibiting wild-type and multidrug-resistant mutated HIV-1 proteases. Biochemistry (2009) 0.85

Vigilance states in a parkinsonian model, the MPTP mouse. Eur J Neurosci (2004) 0.85

Dimerization inhibitors of HIV-1 protease. Biol Chem (2002) 0.85

Molecular tongs containing amino acid mimetic fragments: new inhibitors of wild-type and mutated HIV-1 protease dimerization. J Med Chem (2006) 0.84

Metal-organic compounds: a new approach for drug discovery. N1-(4-methyl-2-pyridyl)-2,3,6-trimethoxybenzamide copper(II) complex as an inhibitor of human immunodeficiency virus 1 protease. Biochem Pharmacol (2002) 0.84

Novel organic proteasome inhibitors identified by virtual and in vitro screening. J Med Chem (2010) 0.83

Regulation of the 26S proteasome activities by peptides mimicking cleavage products. Biochem Biophys Res Commun (2002) 0.83

Cardiovascular protective role for activated protein C during endotoxemia in rats. Intensive Care Med (2006) 0.83

20S proteasome inhibition: designing noncovalent linear peptide mimics of the natural product TMC-95A. ChemMedChem (2010) 0.81

Dimerized linear mimics of a natural cyclopeptide (TMC-95A) are potent noncovalent inhibitors of the eukaryotic 20S proteasome. J Med Chem (2013) 0.81

1,2,4-Triazole derivatives as transient inactivators of kallikreins involved in skin diseases. Bioorg Med Chem Lett (2013) 0.81

Synthesis of new triazole-based trifluoromethyl scaffolds. Beilstein J Org Chem (2008) 0.81

Cyclic RGD-peptidomimetics containing bifunctional diketopiperazine scaffolds as new potent integrin ligands. Chemistry (2009) 0.81

α- and β-hydrazino acid-based pseudopeptides inhibit the chymotrypsin-like activity of the eukaryotic 20S proteasome. Eur J Med Chem (2013) 0.80

Analogues of key precursors of aspartyl protease inhibitors: synthesis of trifluoromethyl amino epoxides. J Org Chem (2005) 0.80

Influence of the structure of polyfluorinated alcohols on Brønsted acidity/hydrogen-bond donor ability and consequences on the promoter effect. J Org Chem (2011) 0.80

Linear TMC-95-based proteasome inhibitors. J Med Chem (2007) 0.80

In vitro antileishmanial activity of fluoro-artemisinin derivatives against Leishmania donovani. Biomed Pharmacother (2008) 0.80

Fluoroartemisinin: trifluoromethyl analogues of artemether and artesunate. J Med Chem (2004) 0.79

Stereoselective Barbier-type allylation reaction of trifluoromethyl aldimines. J Org Chem (2003) 0.79

Development of lipopeptides for inhibiting 20S proteasomes. Bioorg Med Chem Lett (2006) 0.78

Thyroxine-derivatives of lipopeptides: bifunctional dimerization inhibitors of human immunodeficiency virus-1 protease. Biochem Pharmacol (2003) 0.78

Dimerization inhibitors of HIV-1 protease based on a bicyclic guanidinium subunit. J Med Chem (2003) 0.78

Toward the first nonpeptidic molecular tong inhibitor of wild-type and mutated HIV-1 protease dimerization. ChemMedChem (2010) 0.78

Alkylation of manganese(II) tetraphenylporphyrin by antimalarial fluorinated artemisinin derivatives. Bioorg Med Chem Lett (2003) 0.78

Synthesis and cytotoxic activity of fluorinated analogues of Goniothalamus lactones. Impact of fluorine on oxidative processes. Eur J Med Chem (2010) 0.78

Nonmetal catalyzed insertion reactions of diazocarbonyls to acid derivatives in fluorinated alcohols. Org Lett (2011) 0.78

Noncovalent inhibition of 20S proteasome by pegylated dimerized inhibitors. Eur J Med Chem (2012) 0.78

Sugar-based peptidomimetics inhibit amyloid β-peptide aggregation. Eur J Med Chem (2011) 0.77

New constrained "molecular tongs" designed to dissociate HIV-1 protease dimer. J Med Chem (2004) 0.77

Toward the first class of suicide inhibitors of kallikreins involved in skin diseases. J Med Chem (2014) 0.77

Synthesis and conformational studies of pseudopeptides containing an unsymmetrical triazine scaffold. J Pept Sci (2008) 0.77

Fluorous tagging of DABCO through halogen bonding: recyclable catalyst for the Morita-Baylis-Hillman reaction. Chem Commun (Camb) (2011) 0.77

Noncovalent fluorescent probes of human immuno- and constitutive proteasomes. J Med Chem (2014) 0.76

Synthesis of new artemisinin-derived dimers by self-cross-metathesis reaction. Org Lett (2005) 0.76

Carbonylhydrazide-based molecular tongs inhibit wild-type and mutated HIV-1 protease dimerization. J Med Chem (2012) 0.76

An improved capillary electrophoresis method for in vitro monitoring of the challenging early steps of Aβ1-42 peptide oligomerization: application to anti-Alzheimer's drug discovery. Electrophoresis (2014) 0.76

Non-covalent proteasome inhibitors. Curr Pharm Des (2013) 0.76

Design and synthesis of specific probes for human 5-HT4 receptor dimerization studies. J Med Chem (2005) 0.75

The effect of 10 alpha-trifluoromethylhydroartemisinin on Plasmodium berghei infection and its toxicity in experimental animals. Trans R Soc Trop Med Hyg (2003) 0.75

A new series of N5 derivatives of the 1,1,5-trimethyl furo[3,4-c]pyridine-3,4-dione (cerpegin) selectively inhibits the post-acid activity of mammalian 20S proteasomes. Bioorg Med Chem Lett (2012) 0.75

Preparation of 10-trifluoromethyl artemether and artesunate. Influence of hexafluoropropan-2-ol on substitution reaction. J Org Chem (2003) 0.75

Trifluoromethyl nitrones: from fluoral to optically active hydroxylamines. Org Biomol Chem (2010) 0.75

Reactivity of carbon dioxide in hydrofluoroethers: a facile access to cyclic carbonates. Chem Commun (Camb) (2015) 0.75

Liberation of an N-terminal proline-rich peptide from the cryptic proteinase of fibronectin by auto-proteolysis. Arch Biochem Biophys (2008) 0.75

First synthesis of 10 alpha-(trifluoromethyl)deoxoartemisinin. Org Lett (2002) 0.75

Anhydrodihydroartemisinin and its 10-trifluoromethyl analogue: access to novel d-ring-contracted artemisinin trifluoromethyl ketones. J Org Chem (2002) 0.75

Fluorous 4-N,N-dimethylaminopyridine (DMAP) salts as simple recyclable acylation catalysts. Chemistry (2010) 0.75

S(N)/S(N)' competition: selective access to new 10-fluoro artemisinins. J Org Chem (2006) 0.75

Electrophilic amination of fluoroalkyl groups on azodicarboxylate derivatives. J Org Chem (2015) 0.75

Proteasome inhibitors. Prog Mol Subcell Biol (2002) 0.75

Synthesis of substituted 8-aminoquinolines and phenanthrolines through a Povarov approach. Org Biomol Chem (2010) 0.75

Structural and biological effects of a beta2- or beta3-amino acid insertion in a peptide. Eur J Biochem (2003) 0.75

AZT and AZT-monophosphate prodrugs incorporating HIV-protease substrate fragment: synthesis and evaluation as specific drug delivery systems. Antivir Chem Chemother (2006) 0.75

[Proteasome and proteolysis]. J Soc Biol (2004) 0.75

Identification by in silico and in vitro screenings of small organic molecules acting as reversible inhibitors of kallikreins. Eur J Med Chem (2013) 0.75

Solubility switch of gold nanoparticles through hydrogen bond association. Chem Commun (Camb) (2008) 0.75

Orally active antimalarials: hydrolytically stable derivatives of 10-trifluoromethyl anhydrodihydroartemisinin. J Med Chem (2004) 0.75

C1 and N5 derivatives of cerpegin: synthesis of a new series based on structure-activity relationships to optimize their inhibitory effect on 20S proteasome. Bioorg Med Chem Lett (2013) 0.75