Journal of Medicinal Chemistry

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  Publication Venue For

  • Site-Specific Radiohalogenation of a HER2-Targeted Single-Domain Antibody Fragment Using a Novel Residualizing Prosthetic Agent..  65:15358-15373. 2022
  • Identification of Novel 2,4,5-Trisubstituted Pyrimidines as Potent Dual Inhibitors of Plasmodial Pf GSK3/Pf PK6 with Activity against Blood Stage Parasites In Vitro..  65:13172-13197. 2022
  • Quantitative Structure-Activity Relationship (QSAR) Study Predicts Small-Molecule Binding to RNA Structure..  65:7262-7277. 2022
  • Development of Novel ¹⁸ F-PET Agents for Tumor Hypoxia Imaging..  64:5593-5602. 2021
  • Evaluation of Manassantin A Tetrahydrofuran Core Region Analogues and Cooperative Therapeutic Effects with EGFR Inhibition..  63:6821-6833. 2020
  • Structural Optimizations of Thieno[3,2-b]pyrrole Derivatives for the Development of Metabolically Stable Inhibitors of Chikungunya Virus..  60:3165-3186. 2017
  • Trisubstituted Thieno[3,2-b]pyrrole 5-Carboxamides as Potent Inhibitors of Alphaviruses..  58:9196-9213. 2015
  • Characterization and solubilization of pyrrole-imidazole polyamide aggregates..  55:5425-5432. 2012
  • Identification of a nonbasic, nitrile-containing cathepsin K inhibitor (MK-1256) that is efficacious in a monkey model of osteoporosis..  51:6410-6420. 2008
  • A p-[18F]fluoroethoxyphenyl bicyclic nucleoside analogue as a potential positron emission tomography imaging agent for varicella-zoster virus thymidine kinase gene expression..  50:6627-6637. 2007
  • Design and synthesis of human immunodeficiency virus entry inhibitors: sulfonamide as an isostere for the alpha-ketoamide group..  50:6535-6544. 2007
  • On the intractability of estrogen-related receptor alpha as a target for activation by small molecules..  50:6722-6724. 2007
  • Synthesis and preliminary evaluation of 18F- or 11C-labeled bicyclic nucleoside analogues as potential probes for imaging varicella-zoster virus thymidine kinase gene expression using positron emission tomography..  50:1041-1049. 2007
  • Anti-AIDS agents 69. Moronic acid and other triterpene derivatives as novel potent anti-HIV agents..  49:5462-5469. 2006
  • Synthesis and structure-activity relationship of a novel series of aminoalkylindoles with potential for imaging the neuronal cannabinoid receptor by positron emission tomography..  48:5813-5822. 2005
  • Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRbeta and ERRgamma..  48:3107-3109. 2005
  • Anti-AIDS agents. 60. Substituted 3'R,4'R-di-O-(-)-camphanoyl-2',2'-dimethyldihydropyrano[2,3-f]chromone (DCP) analogues as potent anti-HIV agents..  47:4072-4082. 2004
  • 5-substituted derivatives of 6-halogeno-3-((2-(S)-azetidinyl)methoxy)pyridine and 6-halogeno-3-((2-(S)-pyrrolidinyl)methoxy)pyridine with low picomolar affinity for alpha4beta2 nicotinic acetylcholine receptor and wide range of lipophilicity: potential probes for imaging with positron emission tomography..  47:2453-2465. 2004
  • Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents..  46:2973-2984. 2003
  • Neuromuscular blocking activity and therapeutic potential of mixed-tetrahydroisoquinolinium halofumarates and halosuccinates in rhesus monkeys..  46:2502-2515. 2003
  • Synthesis, structure-activity relationship, and evaluation of SR141716 analogues: development of central cannabinoid receptor ligands with lower lipophilicity..  46:642-645. 2003
  • Anti-AIDS agents 49. Synthesis, anti-HIV, and anti-fusion activities of IC9564 analogues based on betulinic acid..  45:4271-4275. 2002
  • Synthesis and evaluation of a novel series of 2-chloro-5-((1-methyl-2-(S)-pyrrolidinyl)methoxy)-3-(2-(4-pyridinyl)vinyl)pyridine analogues as potential positron emission tomography imaging agents for nicotinic acetylcholine receptors..  45:2841-2849. 2002
  • 3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency..  45:2388-2409. 2002
  • Diguanidino and "reversed" diamidino 2,5-diarylfurans as antimicrobial agents..  44:1741-1748. 2001
  • Anti-AIDS agents. 42. Synthesis and anti-HIV activity of disubstituted (3'R,4'R)-3',4'-di-O-(S)-camphanoyl-(+)-cis-khellactone analogues..  44:664-671. 2001
  • Sulfoxide-containing aromatic nitrogen mustards as hypoxia-directed bioreductive cytotoxins..  43:4160-4168. 2000
  • In vitro and in vivo evaluation of dihydropyrimidinone C-5 amides as potent and selective alpha(1A) receptor antagonists for the treatment of benign prostatic hyperplasia..  43:2703-2718. 2000
  • Erratum: Bis- and mixed-tetrahydroisoquinolinium chlorofumarates: New ultra-short-acting nondepolarizing neuromuscular blockers (Journal of Medicinal Chemistry (1999) 42 (207)).  42:1114. 1999
  • Synthesis and dopaminergic properties of benzo-fused analogues of quinpirole and quinelorane..  42:935-940. 1999
  • Bis- and mixed-tetrahydroisoquinolinium chlorofumarates: new ultra-short-acting nondepolarizing neuromuscular blockers..  42:206-209. 1999
  • N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents..  41:5020-5036. 1998
  • Anti-AIDS agents. 34. Synthesis and structure-activity relationships of betulin derivatives as anti-HIV agents..  41:4648-4657. 1998
  • 2-, 5-, and 6-Halo-3-(2(S)-azetidinylmethoxy)pyridines: synthesis, affinity for nicotinic acetylcholine receptors, and molecular modeling..  41:3690-3698. 1998
  • Synthesis and biological activity of a novel methylamine-bridged enkephalin analogue (MABE): a new route to cyclic peptides and peptidomimetics..  41:2631-2635. 1998
  • Synthesis and evaluation of compounds that facilitate the gastrointestinal absorption of heparin..  41:1163-1171. 1998
  • Novel biologically active nonpeptidic inhibitors of myristoylCoA:protein N-myristoyltransferase..  41:996-1000. 1998
  • Synthesis of C3 heteroatom-substituted azetidinones that display potent cholesterol absorption inhibitory activity..  41:752-759. 1998
  • Design and synthesis of novel imidazole-substituted dipeptide amides as potent and selective inhibitors of Candida albicans myristoylCoA:protein N-myristoyltransferase and identification of related tripeptide inhibitors with mechanism-based antifungal activity..  40:2609-2625. 1997
  • Exceptionally potent antispermatogenic compounds from 8-halogenation of (4aRS,5SR,9bRS)-hexahydroindeno-[1,2-c]pyridines..  40:2111-2112. 1997
  • Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate..  40:1726-1730. 1997
  • Antitumor agents. 172. Synthesis and biological evaluation of novel deacetamidothiocolchicin-7-ols and ester analogs as antitubulin agents..  40:961-966. 1997
  • (Aryloxy)aryl semicarbazones and related compounds: a novel class of anticonvulsant agents possessing high activity in the maximal electroshock screen..  39:3984-3997. 1996
  • Betulinic acid and dihydrobetulinic acid derivatives as potent anti-HIV agents..  39:1016-1017. 1996
  • High-affinity inhibitors of dihydrofolate reductase: antimicrobial and anticancer activities of 7,8-dialkyl-1,3-diaminopyrrolo[3,2-f]quinazolines with small molecular size..  39:892-903. 1996
  • Thiopyranol[2,3,4-c,d]indoles as inhibitors of 5-lipoxygenase, 5-lipoxygenase-activating protein, and leukotriene C4 synthase..  38:4538-4547. 1995
  • Novel thiazole based heterocycles as inhibitors of LFA-1/ICAM-1 mediated cell adhesion..  38:1057-1059. 1995
  • Structure-activity studies of 2,3,4,4a,5,9b-hexahydroindeno[1,2-c]pyridines as antispermatogenic agents for male contraception..  38:753-763. 1995
  • GC sequence specific recognition by an N-formamido, C-terminus-modified and imidazole-containing analogue of netropsin..  37:4073-4075. 1994
  • Anti-AIDS agents. 15. Synthesis and anti-HIV activity of dihydroseselins and related analogs..  37:3947-3955. 1994
  • Conformational analysis, pharmacophore identification, and comparative molecular field analysis of ligands for the neuromodulatory sigma 3 receptor..  37:4109-4117. 1994
  • (4-[18F]fluoro-3-iodobenzyl)guanidine, a potential MIBG analogue for positron emission tomography..  37:3655-3662. 1994
  • 6-Azasteroids: structure-activity relationships for inhibition of type 1 and 2 human 5 alpha-reductase and human adrenal 3 beta-hydroxy-delta 5-steroid dehydrogenase/3-keto-delta 5-steroid isomerase..  37:2352-2360. 1994
  • Plant antitumor agents. 31. The calycopterones, a new class of biflavonoids with novel cytotoxicity in a diverse panel of human tumor cell lines..  37:1465-1470. 1994
  • Thiopyrano[2,3,4-cd]indoles as 5-lipoxygenase inhibitors: synthesis, biological profile, and resolution of 2-[2-[1-(4-chlorobenzyl)-4-methyl-6-[(5-phenylpyridin-2-yl)methoxy]-4,5 -dihydro-1H-thiopyrano[2,3,4-cd]indol-2-yl]ethoxy]butanoic acid..  37:1153-1164. 1994
  • New hexahydroxybiphenyl derivatives as inhibitors of protein kinase C..  37:195-200. 1994
  • (4-[¹⁸ F]fluoro-3-iodobenzyl)guanidine, a potential mibg analogue for positron emission tomography.  37:3655-3662. 1994
  • 6-Azasteroids: potent dual inhibitors of human type 1 and 2 steroid 5 alpha-reductase..  36:4313-4315. 1993
  • Substituted thiopyrano[2,3,4-c,d]indoles as potent, selective, and orally active inhibitors of 5-lipoxygenase. Synthesis and biological evaluation of L-691,816..  36:2771-2787. 1993
  • Synthesis and pharmacological evaluation of 1-phenyl-3-amino-1,2,3,4-tetrahydronaphthalenes as ligands for a novel receptor with sigma-like neuromodulatory activity..  36:2542-2551. 1993
  • Synthesis of human CCK26-33 and CCK-33 related analogues on 2,4-DMBHA and TMBHA..  36:1681-1688. 1993
  • Antitumor agents. 139. Synthesis and biological evaluation of thiocolchicine analogs 5,6-dihydro-6(S)-(acyloxy)- and 5,6-dihydro-6(S)-[(aroyloxy)methyl]-1,2,3-trimethoxy-9-(methylthio)-8H- cyclohepta[a]naphthalen-8-ones as novel cytotoxic and antimitotic agents..  36:544-551. 1993
  • Development of a novel series of styrylquinoline compounds as high-affinity leukotriene D4 receptor antagonists: synthetic and structure-activity studies leading to the discovery of (+-)-3-[[[3-[2-(7-chloro-2-quinolinyl)-(E)-ethenyl]phenyl][[3- (dimethylamino)-3-oxopropyl]thio]methyl]thio]propionic acid..  35:3832-3844. 1992
  • Novel non-cross resistant diaminoanthraquinones as potential chemotherapeutic agents.  35:4259-4263. 1992
  • Design, synthesis, and pharmacological evaluation of ultrashort- to long-acting opioid analgetics..  34:2202-2208. 1991
  • Stereospecific synthesis, assignment of absolute configuration, and biological activity of the enantiomers of 3-[[[3-[2-(7-chloroquinolin-2-yl)-(E)-ethenyl]phenyl] [[3-(dimethylamino)-3-oxopropyl]thio]methyl]thio]propionic acid, a potent and specific leukotriene D4 receptor antagonist..  33:2841-2845. 1990
  • Synthesis and dopamine agonist properties of (+-)-trans-3,4,4a,10b-tetrahydro-4-propyl-2H,5H-[1]benzopyrano [4,3-b]-1,4-oxazin-9-ol and its enantiomers..  33:445-450. 1990
  • Synthesis and receptor affinities of some conformationally restricted analogues of the dopamine D1 selective ligand (5R)-8-chloro-2,3,4,5-tetrahydro-3-methyl-5-phenyl- 1H-3-benzazepin-7-ol..  32:1913-1921. 1989
  • 1,2,4-Trioxanes as potential antimalarial agents..  31:713-716. 1988
  • Cardiotonic agents. 8. Selective inhibitors of adenosine 3',5'-cyclic phosphate phosphodiesterase III. Elaboration of a five-point model for positive inotropic activity..  30:1963-1972. 1987
  • N6-phenyladenosines: pronounced effect of phenyl substituents on affinity for A2 adenosine receptors..  30:954-956. 1987
  • N⁶ -phenyladenosines: Pronounced effect of phenyl substituents on affinity for A₂ adenosine receptors.  30:954-956. 1987
  • Antiinflammatory activity of substituted 6-hydroxypyrimido[2,1-f]purine-2,4,8(1H,3H,9H)-triones. Atypical nonsteroidal antiinflammatory agents..  29:1099-1113. 1986
  • Development of an affinity ligand for purification of alpha 2-adrenoceptors from human platelet membranes..  27:918-921. 1984
  • Erratum: Development of an affinity ligand for purification of α2-adrenoceptors from human platelet membranes (Journal of Medicinal Chemistry (1984) 27, (918)).  27:1753. 1984
  • Synthesis of iodine-125 labeled (+/-)-15-(4-azidobenzyl)carazolol: a potent beta-adrenergic photoaffinity probe..  26:832-838. 1983
  • Synthesis and biological activity of zoapatanol analogues..  26:426-430. 1983
  • New azacannabinoids highly active in the central nervous system..  26:278-280. 1983
  • Novel 17 alpha-chloro-17 beta-sulfinyl steroids as specific inhibitors of sebaceous gland activity: potential antiacne agents..  26:78-85. 1983
  • Synthesis, biological activity, and structure--activity/toxicity relationships of a series of terphenyl analogues of hemicholinium-3 and acetyl-seco-hemicholinium-3. 3..  23:541-545. 1980
  • Synthesis of 11 beta,13 beta- and 13 beta,16 beta-propano steroids: probes of hormonal activity..  22:966-970. 1979
  • Acetylenics. 2. Synthesis and pharmacology of certain N,N-diakyl-3-phenylpropyn-2-amines. Some analogues with tryptamine-like behavioral effects in mice..  21:253-257. 1978
  • Cannabinoids. Synthesis and central nervous system activity of 8-substituted 10-hydroxy-5,5-dimethyl-5H-[1]benzopyrano[4,3-c]pyridine and derivatives..  20:1508-1511. 1977
  • Structure and biological activity of (-)-[3H]dihydroalprenolol, a radioligand for studies of beta-adrenergic receptors..  20:1090-1094. 1977
  • 3-Halo-5,7-dimethylpyrazolo [1,5-a]pyrimidines, a nonbenzodiazepinoid class of antianxiety agents devoid of potentiation of central nervous system depressant effects of ethanol or barbiturates..  20:386-393. 1977
  • Effect of sulfur substitution for the noncarbonyl oxygen in hemicholinium-3 and acetyl-seco-hemicholinium-3. Synthesis, biological activity, and structure-toxicity relationships..  20:59-62. 1977
  • Pharmacological activity of nitroxide analogues of dichloroisoproterenol and propranolol..  19:1254-1256. 1976
  • Synthesis and structure-toxicity relationships of three new stable analogues of acetyl-seco-hemicholinium-3..  19:760-763. 1976
  • Drugs derived from cannabinoids. 2. Basic esters of nitrogen and carbocyclic analogs..  19:454-461. 1976
  • Drugs derived from cannabinoids. 4. Effect of alkyl substitution in sulfur and carbocyclic analogs..  19:552-554. 1976
  • Drugs derived from cannabinoids. 5. Delta 6a, 10a-tetrahydrocannabinol and heterocyclic analogs containing aromatic side chains..  19:461-471. 1976
  • Flavonoids. 8. Synthesis and antifertility and estrogen receptor binding activities of coumarins and delta3-isoflavenes..  18:982-985. 1975