Novel C2–C3′ N-peptide linked macrocyclic taxoids. Part 1: Synthesis and biological activities of docetaxel analogues with a peptide side chain at C3′ Fulltext Access 5 Pages 2005
Carbonic anhydrase inhibitors: Inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with benzo[b]thiophene 1,1-dioxide sulfonamides Fulltext Access 5 Pages 2005
Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT6 receptor antagonists Fulltext Access 5 Pages 2005
Carbonic anhydrase inhibitors: Inhibition of the tumor-associated isozymes IX and XII with a library of aromatic and heteroaromatic sulfonamides Fulltext Access 5 Pages 2005
Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective σ1 ligands. Part 1 Fulltext Access 5 Pages 2005
Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective σ1 ligands. Part 2 Fulltext Access 5 Pages 2005
Synthesis and evaluation of 18F-labeled dopamine D3 receptor ligands as potential PET imaging agents Fulltext Access 5 Pages 2005
Activity and QSAR study of baogongteng A and its derivatives as muscarinic agonists Fulltext Access 5 Pages 2005
Synthesis of [1,2,4]triazolo[1,5-a]pyrazines as adenosine A2A receptor antagonists Fulltext Access 5 Pages 2005
Novel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity Fulltext Access 5 Pages 2005
The discovery of fluoropyridine-based inhibitors of the Factor VIIa/TF complex Fulltext Access 5 Pages 2005
Total and semisynthesis and in vitro studies of both enantiomers of 20-fluorocamptothecin Fulltext Access 5 Pages 2005
Parallel synthesis and biological evaluation of 5,6,7,8-tetrahydrobenzothieno[2,3-d]pyrimidin-4(3H)-one cytotoxic agents selective for p21-deficient cells Fulltext Access 5 Pages 2005
Synthesis and in vitro pharmacological studies of C(4) modified salvinorin A analogues Fulltext Access 5 Pages 2005
An efficient synthesis of argifin: A natural product chitinase inhibitor with chemotherapeutic potential Fulltext Access 5 Pages 2005
Diamino-C,N-diarylpyridine positional isomers as inhibitors of lysophosphatidic acid acyltransferase-β Fulltext Access 5 Pages 2005
The neuroprotective action of JNK3 inhibitors based on the 6,7-dihydro-5H-pyrrolo[1,2-a]imidazole scaffold Fulltext Access 5 Pages 2005
Geometry, topology, and atom-weights assembly descriptors to predicting A1 adenosine receptors agonists Fulltext Access 5 Pages 2005
5-Lipoxygenase inhibitors: convenient synthesis of 4-[3-(4-heterocyclylphenylthio)phenyl]-3,4,5,6-tetrahydro-2H-pyran-4-carboxamide analogues Fulltext Access 5 Pages 2005
Synthesis and evaluation of 3D templates based on a taxane skeleton to circumvent P-glycoprotein-associated multidrug resistance of cancer Fulltext Access 5 Pages 2005
Macrolactonization catalyzed by the terminal thioesterase domain of the nonribosomal peptide synthetase responsible for lichenysin biosynthesis Fulltext Access 5 Pages 2005
Structural elucidation of A-74528, an inhibitor for 2â²,5â²-phosphodiesterase isolated from Streptomyces sp. Fulltext Access 5 Pages 2005
Discovery of potent and selective orally bioavailable β-substituted phenylalanine derived dipeptidyl peptidase IV inhibitors Fulltext Access 5 Pages 2005
Synthesis of a small library of diketopiperazines as potential inhibitors of calpain Fulltext Access 5 Pages 2005
Stereospecific synthesis and mass spectrometry of 5,6-trans-epoxy-8Z,11Z,14Z-eicosatrienoic acid Fulltext Access 5 Pages 2005
Exploiting a basic chemosensitizing pharmacophore hypothesis. Part 1: Synthesis and biological evaluation of novel arylbromide and bicyclic chemosensitizers against drug-resistant malaria parasites Fulltext Access 5 Pages 2005
Synthesis of [18F]SU11248, a new potential PET tracer for imaging cancer tyrosine kinase Fulltext Access 5 Pages 2005
Synthesis and antiamoebic activity of new oxime ether derivatives containing 2-acetylpyridine/2-acetylfuran Fulltext Access 5 Pages 2005
8-Piperazinyl-2,3-dihydropyrrolo[3,2-g]isoquinolines: Potent, selective, orally bioavailable 5-HT1 receptor ligands Fulltext Access 5 Pages 2005
Biphenyl-indanones: Allosteric potentiators of the metabotropic glutamate subtype 2 receptor Fulltext Access 5 Pages 2005
Acetylenic TACE inhibitors. Part 2: SAR of six-membered cyclic sulfonamide hydroxamates Fulltext Access 5 Pages 2005
Ligands with dual vitamin D3-agonistic and androgen-antagonistic activities Fulltext Access 5 Pages 2005
Synthesis and evaluation of tricyclic pyrrolopyrimidinones as dipeptide mimetics: Inhibition of interleukin-1β-converting enzyme Fulltext Access 5 Pages 2005
Discovery of 4-(dimethylamino)quinazolines as potent and selective antagonists for the melanin-concentrating hormone receptor 1 Fulltext Access 5 Pages 2005
3-(2-Aminoethyl)pyridine analogs as α4β2 nicotinic cholinergic receptor ligands Fulltext Access 5 Pages 2005
Synthesis and antibacterial activity of a novel series of DNA gyrase inhibitors: 5-[(E)-2-arylvinyl]pyrazoles Fulltext Access 5 Pages 2005
Analogs of a potent maxi-K potassium channel opener with an improved inhibitory profile toward cytochrome P450 isozymes Fulltext Access 5 Pages 2005
Boro-norleucine as a P1 residue for the design of selective and potent DPP7 inhibitors Fulltext Access 5 Pages 2005
Antiviral 6-amino-quinolones: Molecular basis for potency and selectivity Fulltext Access 5 Pages 2005
2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists Fulltext Access 5 Pages 2005
4-Phenyl-1,2,3,6-tetrahydropyridine, an excellent fragment to improve the potency of PARP-1 inhibitors Fulltext Access 5 Pages 2005
Novel, selective indole-based ECE inhibitors: Lead optimization via solid-phase and classical synthesis Fulltext Access 5 Pages 2005
Correlation of cytotoxic activity of betulinines and their hydroxy analogues Fulltext Access 5 Pages 2005
Hepatitis C virus NS3-4A serine protease inhibitors: SAR of P2′ moiety with improved potency Fulltext Access 5 Pages 2005
2-(2-Furanyl)-7-phenyl[1,2,4]triazolo[1,5-c]pyrimidin-5-amine analogs: Highly potent, orally active, adenosine A2A antagonists. Part 1 Fulltext Access 5 Pages 2005
Design, synthesis and ribosome binding of chloramphenicol nucleotide and intercalator conjugates Fulltext Access 5 Pages 2005
2-(Arylmethyl)-3-substituted quinuclidines as selective α7 nicotinic receptor ligands Fulltext Access 5 Pages 2005
2-Ethoxybenzoxazole as a bioisosteric replacement of an ethyl benzoate group in a human rhinovirus (HRV) capsid binder Fulltext Access 5 Pages 2005
Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP Fulltext Access 5 Pages 2005
Synthesis and antibacterial activity of alkyl derivatives of the glycopeptide antibiotic A40926 and their amides Fulltext Access 5 Pages 2005
Synthesis of novel curcumin mimics with asymmetrical units and their anti-angiogenic activity Fulltext Access 5 Pages 2005
Chemical modification of the naphthoyl 3-position of JWH-015: In search of a fluorescent probe to the cannabinoid CB2 receptor Fulltext Access 5 Pages 2005
Phenylpyrroles, a new chemolibrary virtual screening class of 5-HT7 receptor ligands Fulltext Access 5 Pages 2005
Antibiotics GE23077, novel inhibitors of bacterial RNA polymerase. Part 3: Chemical derivatization Fulltext Access 5 Pages 2005
Identification of potent type I MetAP inhibitors by simple bioisosteric replacement. Part 1: Synthesis and preliminary SAR studies of thiazole-4-carboxylic acid thiazol-2-ylamide derivatives Fulltext Access 5 Pages 2005
Functionalized head-to-head hairpin polyamides: Synthesis, double-stranded DNA-binding activity and affinity Fulltext Access 5 Pages 2005
Discovery and SAR of 4-amino-2-biarylbutylurea MCH 1 receptor antagonists through solid-phase parallel synthesis Fulltext Access 5 Pages 2005
Discovery of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid diamides that increase CFTR mediated chloride transport Fulltext Access 5 Pages 2005
4-Fluorosulfonylpiperidines: Selective 5-HT2A ligands for the treatment of insomnia Fulltext Access 5 Pages 2005
Synthesis and bioactivities of two multiple antigen peptides as potential vaccine against schistosoma Fulltext Access 5 Pages 2005
The development of new isoxazolone based inhibitors of tumor necrosis factor-alpha (TNF-α) production Fulltext Access 5 Pages 2005
3-(2-Ethoxy-4-{4-[3-hydroxy-2-methyl-4-(3-methylbutanoyl)phenoxy]butoxy}phenyl)propanoic acid: a brain penetrant allosteric potentiator at the metabotropic glutamate receptor 2 (mGluR2) Fulltext Access 5 Pages 2005
Synthesis and anthelmintic activity of 7-substituted 3,4a-dimethyl-4a,5a,8a,8b-tetrahydro-6H-pyrrolo[3â²,4â²:4,5]furo[3,2-b]pyridine-6,8(7H)-diones Fulltext Access 5 Pages 2005
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED Fulltext Access 5 Pages 2005
Solid-phase synthesis and antibacterial evaluations of N-demethylvancomycin derivatives Fulltext Access 5 Pages 2005
Discovery and optimisation of potent, selective, ethanolamine inhibitors of bacterial phenylalanyl tRNA synthetase Fulltext Access 5 Pages 2005
Furanyl-1,3-thiazol-2-yl and benzoxazol-5-yl acetic acid derivatives: novel classes of heparanase inhibitor Fulltext Access 5 Pages 2005
The development of monocyclic pyrazolone based cytokine synthesis inhibitors Fulltext Access 5 Pages 2005
(1H-Imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: Further optimisation as highly potent and selective MSK-1-inhibitors Fulltext Access 5 Pages 2005
Structure–activity relationships of arylbenzofuran H3 receptor antagonists Fulltext Access 5 Pages 2005
Redefining the structure–activity relationships of 2,6-methano-3-benzazocines. Part 3: 8-Thiocarboxamido and 8-thioformamido derivatives of cyclazocine Fulltext Access 5 Pages 2005
4-Alkyl and 4,4′-dialkyl 1,2-bis(4-chlorophenyl)pyrazolidine-3,5-dione derivatives as new inhibitors of bacterial cell wall biosynthesis Fulltext Access 5 Pages 2005
In vitro advanced antimycobacterial screening of isoniazid-related hydrazones, hydrazides and cyanoboranes: Part 14 Fulltext Access 5 Pages 2005
Synthesis and biological evaluation of new biphalin analogues with non-hydrazine linkers Fulltext Access 5 Pages 2005
Discovery of novel conformationally constrained tropane-based biaryl and arylacetylene ligands as potent and selective norepinephrine transporter inhibitors and potential antidepressants Fulltext Access 5 Pages 2005
Site-specific immobilization of proteins in a microarray using intein-mediated protein splicing Fulltext Access 5 Pages 2005
1-((S)-γ-Substituted prolyl)-(S)-2-cyanopyrrolidine as a novel series of highly potent DPP-IV inhibitors Fulltext Access 5 Pages 2005
Structure–activity relationship of a series of cyclohexylpiperidines bearing an amide side chain as antagonists of the human melanocortin-4 receptor Fulltext Access 5 Pages 2005
Analogues of the neuroprotective tripeptide Gly-Pro-Glu (GPE): synthesis and structure–activity relationships Fulltext Access 5 Pages 2005
(1H-Imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: A novel class of potent MSK-1-inhibitors Fulltext Access 5 Pages 2005
Deoxyribosyl analogues of methionyl and isoleucyl sulfamate adenylates as inhibitors of methionyl-tRNA and isoleucyl-tRNA synthetases Fulltext Access 5 Pages 2005
Synthesis and biological evaluation of quinoxaline-5,8-diones that inhibit vascular smooth muscle cell proliferation Fulltext Access 5 Pages 2005
Syntheses of NAMDA derivatives inhibiting NO production in BV-2 cells stimulated with lipopolysaccharide Fulltext Access 5 Pages 2005
6-Aryl-4-methylsulfanyl-2H-pyran-2-one-3-carbonitriles as PPAR-γ activators Fulltext Access 5 Pages 2005
(2R)-2-Methylchromane-2-carboxylic acids: Discovery of selective PPARα agonists as hypolipidemic agents Fulltext Access 5 Pages 2005
Synthesis of cationic β-vinyl substituted meso-tetraphenylporphyrins and their in vitro activity against herpes simplex virus type 1 Fulltext Access 5 Pages 2005
Synthesis and biological evaluation of benzothiazole derivatives as potent antitumor agents Fulltext Access 5 Pages 2005
Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy Fulltext Access 5 Pages 2005