Solid-phase synthesis of oligomers carrying several chromophore units linked by phosphodiester backbones Fulltext Access 5 Pages 2008
Design, synthesis and antiproliferative properties of oligomers with chromophore units linked by amide backbones Fulltext Access 5 Pages 2008
Fluoroolefins as amide bond mimics in dipeptidyl peptidase IV inhibitors Fulltext Access 5 Pages 2008
Aryl–indolyl maleimides as inhibitors of CaMKIIδ. Part 3: Importance of the indole orientation Fulltext Access 5 Pages 2008
Aryl–indolyl maleimides as inhibitors of CaMKIIδ. Part 1: SAR of the aryl region Fulltext Access 5 Pages 2008
Tetrazole-biarylpyrazole derivatives as cannabinoid CB1 receptor antagonists Fulltext Access 5 Pages 2008
TIE-2/VEGF-R2 SAR and in vitro activity of C3-acyl dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole analogs Fulltext Access 5 Pages 2008
Synthesis of novel N-diazeniumdiolates based on hyperbranched polyethers Fulltext Access 5 Pages 2008
Discovery of 2-amino-6-carboxamidobenzothiazoles as potent Lck inhibitors Fulltext Access 5 Pages 2008
Investigation of novel 7,8-disubstituted-5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-ones as potent Chk1 inhibitors Fulltext Access 5 Pages 2008
Synthesis and antihyperglycemic activity of novel N-acyl-2-arylethylamines and N-acyl-3-coumarylamines Fulltext Access 5 Pages 2008
Synthesis, anti-HIV-1 activity, and modeling studies of N-3 Boc TSAO compound Fulltext Access 5 Pages 2008
Synthesis of a small library of 2-phenoxy-1,4-naphthoquinone and 2-phenoxy-1,4-anthraquinone derivatives bearing anti-trypanosomal and anti-leishmanial activity Fulltext Access 5 Pages 2008
Investigations of the esterase, phosphatase, and sulfatase activities of the cytosolic mammalian carbonic anhydrase isoforms I, II, and XIII with 4-nitrophenyl esters as substrates Fulltext Access 5 Pages 2008
Pyrazolopyridines as a novel structural class of potent and selective PDE4 inhibitors Fulltext Access 5 Pages 2008
Hepatitis C virus NS3-4A serine protease inhibitors: SAR of new P1 derivatives of SCH 503034 Fulltext Access 5 Pages 2008
Design and synthesis of novel 2-pyridone peptidomimetic falcipain 2/3 inhibitors Fulltext Access 5 Pages 2008
Biaryl and heteroaryl derivatives of SCH 58261 as potent and selective adenosine A2A receptor antagonists Fulltext Access 5 Pages 2008
Discovery of potent and cell-active allosteric dual Akt 1 and 2 inhibitors Fulltext Access 5 Pages 2008
Potency and selectivity of P2/P3-modified inhibitors of cysteine proteases from trypanosomes Fulltext Access 5 Pages 2008
2-Substituted 4-, 5-, and 6-[(1E)-3-oxo-3-phenylprop-1-en-1-yl]pyridazin-3(2H)-ones and 2-substituted 4,5-bis[(1E)-3-oxo-3-phenylprop-1-en-1-yl]pyridazin-3(2H)-ones as potent platelet aggregation inhibitors: Design, synthesis, and SAR studies Fulltext Access 5 Pages 2008
An efficient, simple and expedition synthesis of 1-amidoalkyl-2-naphthols as ‘drug like’ molecules for biological screening Fulltext Access 5 Pages 2008
Acylguanidine inhibitors of β-secretase: Optimization of the pyrrole ring substituents extending into the S1′ substrate binding pocket Fulltext Access 5 Pages 2008
Synthesis and biological activity of phosphatidylinositol-3,4,5-trisphosphorothioate Fulltext Access 5 Pages 2008
The first steps. The attack on the carbonyl carbon of pyridoxal cofactor in pyridoxal-dependent enzymes Fulltext Access 5 Pages 2008
Design and synthesis of substituted 4-oxo-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazine-2-carboxamides, novel HIV-1 integrase inhibitors Fulltext Access 5 Pages 2008
α-Hydroxy amides as a novel class of bradykinin B1 selective antagonists Fulltext Access 5 Pages 2008
A new series of neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase Fulltext Access 5 Pages 2008
Complexation of single strand telomere and telomerase RNA template polyanions by deoxyribonucleic guanidine (DNG) polycations: Plausible anticancer agents Fulltext Access 5 Pages 2008
Block of cyclic nucleotide-gated channels by tetracaine derivatives: Role of apolar interactions at two distinct locations Fulltext Access 5 Pages 2008
(Phenylpiperazinyl)cyclohexylureas: Discovery of α1a/1d-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS) Fulltext Access 5 Pages 2008
Development of CXCR3 antagonists. Part 4: Discovery of 2-amino-(4-tropinyl)quinolines Fulltext Access 5 Pages 2008
Structure-based design, synthesis, and biological evaluation of 1,1-dioxoisothiazole and benzo[b]thiophene-1,1-dioxide derivatives as novel inhibitors of hepatitis C virus NS5B polymerase Fulltext Access 5 Pages 2008
Structure-based design and synthesis of novel macrocyclic pyrazolo[1,5-a] [1,3,5]triazine compounds as potent inhibitors of protein kinase CK2 and their anticancer activities Fulltext Access 5 Pages 2008
Rapid novel divergent synthesis and muscarinic agonist profile of all four optical isomers of N,N,N-trimethyl(6-methyl-1,4-dioxan-2-yl)methanaminium iodide Fulltext Access 5 Pages 2008
Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based HTS assay. Part 5: Modifications of the 2- and 3-positions Fulltext Access 5 Pages 2008
Synthesis and structure–activity relationship studies of tyrosine-based antagonists at the human P2X7 receptor Fulltext Access 5 Pages 2008
Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P1′ permutations Fulltext Access 5 Pages 2008
Design and synthesis of novel potent and selective integrin αvβ3 antagonists—Novel synthetic routes to isoquinolinone, benzoxazinone, and quinazolinone acetates Fulltext Access 5 Pages 2008
Microwave-assisted synthesis and antimicrobial activities of flavonoid derivatives Fulltext Access 5 Pages 2008
Synthesis of genistein derivatives and determination of their protective effects against vascular endothelial cell damages caused by hydrogen peroxide Fulltext Access 5 Pages 2008
1-Aminoindanes as novel motif with potential atypical antipsychotic properties Fulltext Access 5 Pages 2008
Design and SAR of selective T-type calcium channel antagonists containing a biaryl sulfonamide core Fulltext Access 5 Pages 2008
Novel 5-HT1A/1B/1D receptors antagonists with potent 5-HT reuptake inhibitory activity Fulltext Access 5 Pages 2008
Site-specific self-cleavage of G-quadruplexes formed by human telemetric repeats Fulltext Access 5 Pages 2008
Discovery of 4-aryl-2-oxo-2H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay Fulltext Access 5 Pages 2008
Optimization and structure–activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: Identification of MK-0873, a potent and effective PDE4 inhibitor Fulltext Access 5 Pages 2008
Discovery, SAR and X-ray structure of 1H-benzimidazole-5-carboxylic acid cyclohexyl-methyl-amides as inhibitors of inducible T-cell kinase (Itk) Fulltext Access 5 Pages 2008
Optimization of a series of potent and selective ketone histone deacetylase inhibitors Fulltext Access 5 Pages 2008
Eicosapentaenoic-acid-derived isoprostanes: Synthesis and discovery of two major isoprostanes Fulltext Access 5 Pages 2008
Synthesis and use of sulfonamide-, sulfoxide-, or sulfone-containing aminoglycoside–CoA bisubstrates as mechanistic probes for aminoglycoside N-6′-acetyltransferase Fulltext Access 5 Pages 2008
Synthesis and antibacterial activity of 4â³-O-heteroarylcarbamoyl derivatives of macrolide Fulltext Access 5 Pages 2008
Discovery of small molecule agonists for the bombesin receptor subtype 3 (BRS-3) based on an omeprazole lead Fulltext Access 5 Pages 2008
Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas—The effect of capping the distal basic piperidine nitrogen Fulltext Access 5 Pages 2008
Discovery of a highly orally bioavailable c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid as a potent hypoglycemic and hypolipidemic agent Fulltext Access 5 Pages 2008
Use of the X-ray structure of the β2-adrenergic receptor for drug discovery. Part 2: Identification of active compounds Fulltext Access 5 Pages 2008
Identification of novel inhibitors of extracellular signal-regulated kinase 2 based on the structure-based virtual screening Fulltext Access 5 Pages 2008
Engineering of avermectin biosynthetic genes to improve production of ivermectin in Streptomyces avermitilis Fulltext Access 5 Pages 2008
The ‘Ethereal’ nature of TLR4 agonism and antagonism in the AGP class of lipid A mimetics Fulltext Access 5 Pages 2008
Catalytic site-selective synthesis and evaluation of a series of erythromycin analogs Fulltext Access 5 Pages 2008
Two-color labeling of temporally defined protein populations in mammalian cells Fulltext Access 5 Pages 2008
Chemical probes for profiling fatty acid-associated proteins in living cells Fulltext Access 5 Pages 2008
Development of bestatin-based activity-based probes for metallo-aminopeptidases Fulltext Access 5 Pages 2008
Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics Fulltext Access 5 Pages 2008
Discovery of inhibitors of the channel-activating protease prostasin (CAP1/PRSS8) utilizing structure-based design Fulltext Access 5 Pages 2008
Evaluating the potential of Vacuolar ATPase inhibitors as anticancer agents and multigram synthesis of the potent salicylihalamide analog saliphenylhalamide Fulltext Access 5 Pages 2008
Urotensin-II receptor antagonists: Synthesis and SAR of N-cyclic azaalkyl benzamides Fulltext Access 5 Pages 2008
Novel fluorinated acridone derivatives. Part 1: Synthesis and evaluation as potential anticancer agents Fulltext Access 5 Pages 2008
Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 1: Identification of dipeptide derived leads Fulltext Access 5 Pages 2008
Discovery of a potent and selective c-Kit inhibitor for the treatment of inflammatory diseases Fulltext Access 5 Pages 2008
Enantioselective synthesis of (R)-(+)- and (S)-(−)-higenamine and their analogues with effects on platelet aggregation and experimental animal model of disseminated intravascular coagulation Fulltext Access 5 Pages 2008
Discovery of conformationally rigid 3-azabicyclo[3.1.0]hexane-derived dipeptidyl peptidase-IV inhibitors Fulltext Access 5 Pages 2008
N-(2,2-Dimethyl-2-(2-nitrophenyl)acetyl)-4-aminocyclophosphamide as a potential bioreductively activated prodrug of phosphoramide mustard Fulltext Access 5 Pages 2008
Discovery of novel 1,2,3,4-tetrahydroisoquinolines and 3,4-dihydroisoquinoline-1(2H)-ones as potent and selective inhibitors of KDR: Synthesis, SAR, and pharmacokinetic properties Fulltext Access 5 Pages 2008
Structure, antimicrobial activity and DNA-binding properties of the cobalt(II)–sparfloxacin complex Fulltext Access 5 Pages 2008
Discovery of new Gram-negative antivirulence drugs: Structure and properties of novel E. coli WaaC inhibitors Fulltext Access 5 Pages 2008
Synthesis and biological evaluation of trisubstituted imidazole derivatives as inhibitors of p38α mitogen-activated protein kinase Fulltext Access 5 Pages 2008
A serine protease inhibitor from hemolymph of green mussel, Perna viridis Fulltext Access 5 Pages 2008
Quantitating the concentration of Py-Im polyamide–fluorescein conjugates in live cells Fulltext Access 5 Pages 2008
Facile synthesis, ex-vivo and in vitro screening of 3-sulfonamide derivative of 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide (SR141716) a potent CB1 receptor antagonist Fulltext Access 5 Pages 2008
Synthesis and discovery of autophagy inducers for A549 and H460 lung cancer cells, novel 1-(2′-hydroxy-3′-aroxypropyl)-3-aryl-1H-pyrazole-5-carbohydrazide derivatives Fulltext Access 5 Pages 2008
Identification and SAR around N-{2-[4-(2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-[1,4]diazepan-1-yl]-ethyl}-2-phenoxy-nicotinamide, a selective α2C adrenergic receptor antagonist Fulltext Access 5 Pages 2008
Design, synthesis and antiviral efficacy of a series of potent chloropyridyl ester-derived SARS-CoV 3CLpro inhibitors Fulltext Access 5 Pages 2008
Design and synthesis of 2-amino-pyrazolopyridines as Polo-like kinase 1 inhibitors Fulltext Access 5 Pages 2008
Synthesis and activity of substituted carbamates as potentiators of the α4β2 nicotinic acetylcholine receptor Fulltext Access 5 Pages 2008
Novel HCV NS5B polymerase inhibitors derived from 4-(1′,1′-dioxo-1′,4′-dihydro-1′λ6-benzo[1′,2′,4′]thiadiazin-3′-yl)-5-hydroxy-2H-pyridazin-3-ones. Part 5: Exploration of pyridazinones containing 6-amino-substituents Fulltext Access 5 Pages 2008
Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4): Part I. Discovery of pyrazolo[3,4-d]pyrimidines as novel mGluR4 positive allosteric modulators Fulltext Access 5 Pages 2008
Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1 Fulltext Access 5 Pages 2008