Bioorganic & Medicinal Chemistry Letters
-
Publication Venue For
-
Conversion of carbazole carboxamide based reversible inhibitors of Bruton's tyrosine kinase (BTK) into potent, selective irreversible inhibitors in the carbazole, tetrahydrocarbazole, and a new 2,3-dimethylindole series..
28:3080-3084.
2018
-
Synthetic efforts towards the stereoselective synthesis of NF00659B1..
28:2746-2750.
2018
-
The hydrolytic susceptibility of prochelator BSIH in aqueous solutions..
27:4165-4170.
2017
-
Drug-like property-driven optimization of 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against rilpivirine-resistant mutant virus..
27:2788-2792.
2017
-
A multifunctional, light-activated prochelator inhibits UVA-induced oxidative stress..
25:4843-4847.
2015
-
Structure-activity relationship studies of QS11, a small molecule Wnt synergistic agonist..
25:4838-4842.
2015
-
Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton's tyrosine kinase (BTK) and Janus kinase 2 (JAK2)..
25:4265-4269.
2015
-
Evaluation of class I HDAC isoform selectivity of largazole analogues..
24:3728-3731.
2014
-
Discovery of novel bacterial elongation condensing enzyme inhibitors by virtual screening..
24:2585-2588.
2014
-
Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases..
24:2206-2211.
2014
-
Fluorescence detection of cationic amyloid fibrils in human semen..
23:5199-5202.
2013
-
An enthalpic basis of additivity in biphenyl hydroxamic acid ligands for stromelysin-1..
22:6521-6524.
2012
-
Novel tricyclic inhibitors of IKK2: discovery and SAR leading to the identification of 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066)..
21:7006-7012.
2011
-
A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold..
21:4164-4169.
2011
-
Synthesis and SAR of pyrimidine-based, non-nucleotide P2Y14 receptor antagonists..
21:2832-2835.
2011
-
The identification of 4,7-disubstituted naphthoic acid derivatives as UDP-competitive antagonists of P2Y14..
21:2836-2839.
2011
-
Difluoroethylamines as an amide isostere in inhibitors of cathepsin K..
21:920-923.
2011
-
Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis..
21:383-386.
2011
-
Investigation of 4-piperidinols as novel H3 antagonists.
20:6246-6249.
2010
-
2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors..
20:1724-1727.
2010
-
Synthesis of 4'-ester analogs of resveratrol and their evaluation in malignant melanoma and pancreatic cell lines..
20:1198-1201.
2010
-
The discovery of MK-0674, an orally bioavailable cathepsin K inhibitor..
20:887-892.
2010
-
A single step purification for autolytic zinc proteinases..
20:280-282.
2010
-
Structure-activity relationship study of EphB3 receptor tyrosine kinase inhibitors..
19:6122-6126.
2009
-
Corrigendum to "Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding" [Bioorg. Med. Chem. Lett. 19 (2009) 1694] (DOI:10.1016/j.bmcl.2009.01.094).
19:2604.
2009
-
Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IkappaB kinase..
19:2646-2649.
2009
-
Design, synthesis, and structure–activity relationship study of a novel class of ORL1 receptor antagonists based on N-biarylmethyl spiropiperidine.
18:3778-3782.
2008
-
Discovery of [(3-bromo-7-cyano-2-naphthyl)(difluoro)methyl]phosphonic acid, a potent and orally active small molecule PTP1B inhibitor..
18:3200-3205.
2008
-
Novel ORL1-selective antagonists with oral bioavailability and brain penetrability.
18:3282-3285.
2008
-
Facile synthesis of substituted trans-2-arylcyclopropylamine inhibitors of the human histone demethylase LSD1 and monoamine oxidases A and B..
18:3047-3051.
2008
-
Substituted 2,2-bisaryl-bicycloheptanes as novel and potent inhibitors of 5-lipoxygenase activating protein..
18:2023-2027.
2008
-
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K..
18:923-928.
2008
-
Synthesis and evaluation of a phosphonate analogue of the soluble guanylate cyclase activator YC-1..
17:4938-4941.
2007
-
Synthesis and structure-activity relationship of imidazo(1,2-a)thieno(3,2-e)pyrazines as IKK-beta inhibitors..
17:4284-4289.
2007
-
Synthesis and biological evaluation of an 123I-labeled bicyclic nucleoside analogue (BCNA) as potential SPECT tracer for VZV-tk reporter gene imaging..
17:3458-3462.
2007
-
Synthesis and biological evaluation of 4-amino derivatives of benzimidazoquinoxaline, benzimidazoquinoline, and benzopyrazoloquinazoline as potent IKK inhibitors..
17:1233-1237.
2007
-
Quantitative structure-activity relationship (QSAR) of indoloacetamides as inhibitors of human isoprenylcysteine carboxyl methyltransferase..
17:1025-1032.
2007
-
Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series..
16:4686-4691.
2006
-
Synthesis of Hsp90 dimerization modulators..
16:3529-3532.
2006
-
Identification of a potent and selective non-basic cathepsin K inhibitor..
16:1985-1989.
2006
-
Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma..
16:821-824.
2006
-
Structure-activity relationship studies of salubrinal lead to its active biotinylated derivative..
15:3849-3852.
2005
-
Synthesis of the optical isomers of a new anticholinergic drug, penehyclidine hydrochloride (8018)..
15:1979-1982.
2005
-
The identification and optimization of a N-hydroxy urea series of flap endonuclease 1 inhibitors.
15:277-281.
2005
-
The identification and optimization of 2,4-diketobutyric acids as flap endonuclease 1 inhibitors.
14:4915-4918.
2004
-
Synthesis of a novel peptidic photoaffinity probe for the PTP-1B enzyme..
14:2319-2322.
2004
-
Structure–activity relationships of a novel class of endothelin receptor selective antagonists; 6-carboxy-2-isopropylamino-5,7-diarylcyclopenteno[1,2-b]pyridines.
14:1503-1507.
2004
-
Structure based design of a series of potent and selective non peptidic PTP-1B inhibitors..
14:1043-1048.
2004
-
3,4-Diaryl-5-hydroxyfuranones: highly selective inhibitors of cyclooxygenase-2 with aqueous solubility..
13:1195-1198.
2003
-
Pyridazinones as selective cyclooxygenase-2 inhibitors..
13:597-600.
2003
-
Synthesis and NK(1)/NK(2) binding activities of a series of diacyl-substituted 2-arylpiperazines..
12:3161-3165.
2002
-
Antitumor agents. Part 215: antitubulin effects of cytotoxic B-ring modified allocolchicinoids..
12:2851-2853.
2002
-
Cytotoxic, antifouling bromotyramines: a synthetic study on simple marine natural products and Their analogues..
12:823-825.
2002
-
New series of aryloxypropanolamines with both human beta(3)-adrenoceptor agonistic activity and free radical scavenging properties..
12:209-212.
2002
-
Synthesis of P(1)-Citronellyl-P(2)-alpha-D-pyranosyl pyrophosphates as potential substrates for the E. coli undecaprenyl-pyrophosphoryl-N-acetylglucoseaminyl transferase MurG..
11:3107-3110.
2001
-
Synthesis and separation of diastereomers of uridine 2',3'-cyclic boranophosphate..
11:615-617.
2001
-
Non-peptidic, non-prenylic inhibitors of the prenyl protein-specific protease Rce1..
11:425-427.
2001
-
Synthesis, characterization, and activity of metabolites derived from the cyclooxygenase-2 inhibitor rofecoxib (MK-0966, Vioxx)..
10:2683-2686.
2000
-
Synthesis and biological activity of a novel series of indole-derived PPARgamma agonists..
9:3329-3334.
1999
-
A new structural variation on the methanesulfonylphenyl class of selective cyclooxygenase-2 inhibitors..
9:3181-3186.
1999
-
Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors..
9:3187-3192.
1999
-
Synthesis and biological characterization of sqbazide, a novel biotinylated photoaffinity probe for the study of the human platelet thromboxane A2 receptor..
9:2963-2968.
1999
-
Substituted indoles as potent and orally active 5-lipoxygenase activating protein (FLAP) inhibitors..
9:2391-2396.
1999
-
The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor..
9:1773-1778.
1999
-
Synthesis and cytotoxicity of acetyl-4H,9H-naphtho[2,3-b]thiophene-4,9-diones..
8:2763-2768.
1998
-
Synthesis and creatine kinase inhibitory activity of nonhydrolyzable analogs of phosphocreatine.
7:1021-1026.
1997
-
Dicarboxylic acid inhibitors of phospholipase A2.
7:793-798.
1997
-
A new series of selective COX-2 inhibitors: 5,6-diarylthiazolo[3,2-b][1,2,4]triazoles.
7:57-62.
1997
-
Synthesis and biological evaluation of 5,6-diarylimidazo[2.1-b]thiazole as selective COX-2 inhibitors.
7:47-52.
1997
-
(-)-SCH 57939: Synthesis and pharmacological properties of a potent, metabolically stable cholesterol absorption inhibitor.
6:2069-2072.
1996
-
Stereoselective synthesis and biological activity of cis azetidinones as cholesterol absorption inhibitors.
6:1947-1950.
1996
-
Target directed enediyne prodrugs: hER and AhR degradation by a synthetic oxo-enediyne.
6:1971-1976.
1996
-
Substituted morpholine-2S-acetic acid derivatives: SCH 50911 and related compounds as novel GABA(B) antagonists.
6:1529-1534.
1996
-
Direct characterization of solid phase resin-bound molecules by mass spectrometry.
6:979-982.
1996
-
A cembranolide diterpene farnesyl protein transferase inhibitor from the marine soft coral Lobophytum cristagalli.
6:909-912.
1996
-
Synthesis and evaluation of pyrazolo[3,4-b]quinoline ribofuranosides and their derivatives as inhibitors of oncogenic Ras.
6:195-200.
1996
-
3′,4′-Di-o-(-)-camphanoyl-(+)-ciskhellactone and related compounds: A. new class of potent anti-HIV agents.
4:593-598.
1994
-
Justicidin E: A new leukotriene biosynthesis inhibitor..
3:2063-2066.
1993
-
Novel, stereoselective syntheses of penem antibiotics: efficient, formal syntheses of SCH 34343.
3:2171-2176.
1993
-
Synthesis and absolute configuration of hydroxythreonine, a biosynthetic precursor of rhizobitoxine in pseudomonas.
3:2095-2098.
1993
-
New hexahydroxydiphenyl derivatives as potent inhibitors of HIV replication in H9 lymphocytes.
2:235-238.
1992
-
A new class of leukotriene biosynthesis inhibitors: The development of ((4-(4-chlorophenyl)-1-(4-(2-quinolinylmethoxy)phenyl)butyl)thio)acetic acid, L-674,636.
1:645-648.
1991