Paul W Erhardt
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Distinguished University Professor Emeritus
Professor, University of Toledo
Contact Info
Publications
selected publications
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Article (Faculty180)
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2001Mechanistic considerations pertaining to the solvolysis of paclitaxel analogs bearing ester groups at the C2' position. Tetrahedron letters. 42:7747-7750.
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Article (Web of Science)
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2021Synthesis and Evaluation of PPAR delta Agonists That Promote Osteogenesis in a Human Mesenchymal Stem Cell Culture and in a Mouse Model of Human Osteoporosis. JOURNAL OF MEDICINAL CHEMISTRY. 64:6996-7032.Full Text via DOI: 10.1021/acs.jmedchem.1c00560 PMID: 33988379
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2021Glossary and tutorial of xenobiotic metabolism terms used during small molecule drug discovery and development (IUPAC Technical Report). PURE AND APPLIED CHEMISTRY. 93:273-403.Full Text via DOI: 10.1515/pac-2018-0208
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2020Repurposing metformin, simvastatin and digoxin as a combination for targeted therapy for pancreatic ductal adenocarcinoma. CANCER LETTERS. 491:97-107.Full Text via DOI: 10.1016/j.canlet.2020.08.002 PMID: 32829010
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2020Investigating the Potential to Deliver and Maintain Plasma and Brain Levels of a Novel Practically Insoluble Methuosis Inducing Anticancer Agent 5-Methoxy MOMIPP Through an Injectable In Situ Forming Thermoresponsive Hydrogel Formulation. JOURNAL OF PHARMACEUTICAL SCIENCES. 109:2719-2728.Full Text via DOI: 10.1016/j.xphs.2020.05.014 PMID: 32473210
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2020Bilirubin remodels murine white adipose tissue by reshaping mitochondrial activity and the coregulator profile of peroxisome proliferator–activated receptor α. JOURNAL OF BIOLOGICAL CHEMISTRY. 295:9804-9822.Full Text via DOI: 10.1074/jbc.ra120.013700
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20196-MOMIPP, a novel brain-penetrant anti-mitotic indolyl-chalcone, inhibits glioblastoma growth and viability. CANCER CHEMOTHERAPY AND PHARMACOLOGY. 83:237-254.Full Text via DOI: 10.1007/s00280-018-3726-1
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2019The JNK signaling pathway plays a key role in methuosis (non-apoptotic cell death) induced by MOMIPP in glioblastoma. BMC CANCER. 19.Full Text via DOI: 10.1186/s12885-019-5288-y
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2019BIRC5 is a target for molecular imaging and detection of human pancreatic cancer. CANCER LETTERS. 457:10-19.Full Text via DOI: 10.1016/j.canlet.2019.04.036 PMID: 31059751
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2017Leukocyte integrin Mac-1 regulates thrombosis via interaction with platelet GPIb alpha. NATURE COMMUNICATIONS. 8.Full Text via DOI: 10.1038/ncomms15559
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2016Cytochrome P-450, CYP93A1, as defense marker in soybean. BIOLOGIA PLANTARUM. 60:724-730.Full Text via DOI: 10.1007/s10535-016-0629-z
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2016Synthesis and biological evaluation of isomeric methoxy substitutions on anti-cancer indolyl-pyridinyl-propenones: Effects on potency and mode of activity. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. 122:79-91.Full Text via DOI: 10.1016/j.ejmech.2016.06.016
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2015Total Synthesis of (+/-)-Glyceollin II and a Dihydro Derivative. JOURNAL OF NATURAL PRODUCTS. 78:2940-2947.Full Text via DOI: 10.1021/acs.jnatprod.5b00607
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2015Synthesis and Biological Evaluation of Indolyl-Pyridinyl-Propenones Having Either Methuosis or Microtubule Disruption Activity. JOURNAL OF MEDICINAL CHEMISTRY. 58:2489-2512.Full Text via DOI: 10.1021/jm501997q
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2014Differential Induction of Cytoplasmic Vacuolization and Methuosis by Novel 2-Indolyl-Substituted Pyridinylpropenones. ACS MEDICINAL CHEMISTRY LETTERS. 5:73-77.Full Text via DOI: 10.1021/ml4003925
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2013Synthesis of 6a-hydroxypterocarpans via intramolecular benzoin condensation. TETRAHEDRON LETTERS. 54:4121-4124.Full Text via DOI: 10.1016/j.tetlet.2013.05.121
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2013Practical synthesis of a chromene analog for use as a retinoic acid receptor alpha antagonist lead compound. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. 63:104-108.Full Text via DOI: 10.1016/j.ejmech.2013.02.012
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2013Glossary of terms used in medicinal chemistry. Part II (IUPAC Recommendations 2013). PURE AND APPLIED CHEMISTRY. 85:1725-1758.Full Text via DOI: 10.1351/PAC-REC-12-11-23
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2013Glossary of terms used in medicinal chemistry. Part II (IUPAC Recommendations 2013). PURE AND APPLIED CHEMISTRY. 85:1725-1758.Full Text via DOI: 10.1351/pac-rec-12-11-23
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2012Glyceollins, Soy Isoflavone Phytoalexins, Improve Oral Glucose Disposal by Stimulating Glucose Uptake. JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY. 60:6376-6382.Full Text via DOI: 10.1021/jf301057d
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2012Early Stage Efficacy and Toxicology Screening for Antibiotics and Enzyme Inhibitors. JOURNAL OF BIOMOLECULAR SCREENING. 17:673-682.Full Text via DOI: 10.1177/1087057112438769
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2012On the Interaction of Aliphatic Amines and Ammonium Ions with Carboxylic Acids in Solution and in Receptor Pockets. JOURNAL OF PHYSICAL CHEMISTRY B. 116:5425-5436.Full Text via DOI: 10.1021/jp300588q
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2012Molecular docking and enzymatic evaluation to identify selective inhibitors of aspartate semialdehyde dehydrogenase. BIOORGANIC & MEDICINAL CHEMISTRY. 20:2950-2956.Full Text via DOI: 10.1016/j.bmc.2012.03.013
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2012Synthesis and Evaluation of Indole-Based Chalcones as Inducers of Methuosis, a Novel Type of Nonapoptotic Cell Death. JOURNAL OF MEDICINAL CHEMISTRY. 55:1940-1956.Full Text via DOI: 10.1021/jm201006x
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2012Analogue-based drug discovery: Contributions to medicinal chemistry principles and drug design strategies. Microtubule stabilizers as a case in point (Special Topic Article). PURE AND APPLIED CHEMISTRY. 84:1479-1542.Full Text via DOI: 10.1351/PAC-CON-12-02-13
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2012HITTING A SOFT DRUG WITH A HARD NUCLEOPHILE: PREPARATION OF ESMOLOL'S METABOLITE BY TREATMENT WITH BIS(TRIBUTYLTIN) OXIDE. SYNTHETIC COMMUNICATIONS. 42:722-726.Full Text via DOI: 10.1080/00397911.2010.530375
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2012Analogue-based drug discovery: Contributions to medicinal chemistry principles and drug design strategies. Microtubule stabilizers as a case in point (Special Topic Article). PURE AND APPLIED CHEMISTRY. 84:1479-1542.Full Text via DOI: 10.1351/pac-con-12-02-13
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2011Hypoxia Activated Prodrugs of a 9-Aza-anthrapyrazole Derivative That Has Promising Anticancer Activity. JOURNAL OF MEDICINAL CHEMISTRY. 54:8224-8227.Full Text via DOI: 10.1021/jm200984x
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2011Multigram Synthesis of Glyceollin I. ORGANIC PROCESS RESEARCH & DEVELOPMENT. 15:1149-1162.Full Text via DOI: 10.1021/op200112g
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2011Total Syntheses of (+/-)-Vestitol and Bolusanthin III Using a Wittig Strategy. SYNLETT. 1605-1607.Full Text via DOI: 10.1055/s-0030-1260783
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2011Biomimetic Syntheses and Antiproliferative Activities of Racemic, Natural (-), and Unnnatural (+) Glyceollin I. JOURNAL OF MEDICINAL CHEMISTRY. 54:3506-3523.Full Text via DOI: 10.1021/jm101619e
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2011Syntheses of 2,3-Diarylated 2H-Benzo[e][1,2]Thiazine 1,1-Dioxides and their 3,4-Dihydro Derivatives, and Assessment of their Inhibitory Activity Against MCF-7 Breast Cancer Cells. MEDICINAL CHEMISTRY. 7:561-571.Full Text via DOI: 10.2174/157340611797928307
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2010Theoretical Studies of Salt-Bridge Formation by Amino Acid Side Chains in Low and Medium Polarity Environments. JOURNAL OF PHYSICAL CHEMISTRY B. 114:16436-16442.Full Text via DOI: 10.1021/jp103313s
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2010Glyceollin I enantiomers distinctly regulate ER-mediated gene expression. STEROIDS. 75:870-878.Full Text via DOI: 10.1016/j.steroids.2010.05.007
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2010Determination of esmolol and metabolite enantiomers within human plasma using chiral column chromatography. JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES. 878:2449-2452.Full Text via DOI: 10.1016/j.jchromb.2010.07.006
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2009Total Syntheses of Racemic and Natural Glycinol. JOURNAL OF NATURAL PRODUCTS. 72:2072-2075.Full Text via DOI: 10.1021/np900509f
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2009Monte Carlo structure simulations for tertiary-butyl alcohol solutions in water/acetonitrile solvents. JOURNAL OF MOLECULAR STRUCTURE-THEOCHEM. 895:116-126.Full Text via DOI: 10.1016/j.theochem.2008.10.026
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2008Total Syntheses of Racemic, Natural (-) and Unnatural (+) Glyceollin I.. ORGANIC LETTERS. 10:5007-5010.Full Text via DOI: 10.1021/ol802112r
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2008Catalytically active peptidylglycine alpha-amidating monooxygenase in the media of androgen-independent prostate cancer cell lines. JOURNAL OF BIOMOLECULAR SCREENING. 13:804-809.Full Text via DOI: 10.1177/1087057108321976
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2008Rapid and sensitive HPLC assay for simultaneous determination of procaine and para-aminobenzoic acid from human and rat liver tissue extracts. JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES. 867:247-252.Full Text via DOI: 10.1016/j.jchromb.2008.04.014
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2008Ab initio study of hydrogen-bond formation between aliphatic and phenolic hydroxy groups and selected amino acid side chains. JOURNAL OF PHYSICAL CHEMISTRY A. 112:4342-4354.Full Text via DOI: 10.1021/jp7108847
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2008Practical synthesis of lespedezol A(1). JOURNAL OF NATURAL PRODUCTS. 71:275-277.Full Text via DOI: 10.1021/np070493m
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2007Total synthesis of xanthohumol. JOURNAL OF NATURAL PRODUCTS. 70:1507-1509.Full Text via DOI: 10.1021/np070158y
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2007Simultaneous determination of procaine and para-aminobenzoic acid by LC-MS/MS method. JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES. 847:224-230.Full Text via DOI: 10.1016/j.jchromb.2006.10.004
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2007Rapid and simultaneous determination of capecitabine and its metabolites in mouse plasma, mouse serum, and in rabbit bile by high-performance liquid chromatography. JOURNAL OF CHROMATOGRAPHY A. 1138:101-108.Full Text via DOI: 10.1016/j.chroma.2006.10.038
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2006Ab initio study of hydrogen-bond formation between cyclic ethers and selected amino acid side chains. JOURNAL OF PHYSICAL CHEMISTRY A. 110:13923-13932.Full Text via DOI: 10.1021/jp061113t
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2006Antiestrogenic glyceollins suppress human breast and ovarian carcinoma tumorigenesis. CLINICAL CANCER RESEARCH. 12:7159-7164.Full Text via DOI: 10.1158/1078-0432.CCR-06-1426
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2006Simultaneous determination of vinclozolin and detection of its degradation products in mouse plasma, serum and urine, and from rabbit bile, by high-performance liquid chromatography. JOURNAL OF CHROMATOGRAPHY A. 1115:8-18.Full Text via DOI: 10.1016/j.chroma.2006.02.062
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2006Antiestrogenic Glyceollins Suppress Human Breast and Ovarian Carcinoma Tumorigenesis. CLINICAL CANCER RESEARCH. 12:7159-7164.Full Text via DOI: 10.1158/1078-0432.ccr-06-1426
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2005Monte Carlo simulations of the solution structure of simple alcohols in water-acetonitrile mixtures. JOURNAL OF PHYSICAL CHEMISTRY B. 109:5855-5872.
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2005Monte Carlo Simulations of the Solution Structure of Simple Alcohols in Water−Acetonitrile Mixtures. JOURNAL OF PHYSICAL CHEMISTRY B. 109:5855-5872.Full Text via DOI: 10.1021/jp045570q
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2002Microplate Screening of the Differential Effects of Test Agents on Hoechst 33342, Rhodamine 123, and Rhodamine 6G Accumulation in Breast Cancer Cells that Overexpress P–Glycoprotein. JOURNAL OF BIOMOLECULAR SCREENING. 7:29-34.Full Text via DOI: 10.1089/108705702753520314
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2002SELECTIVE CONVERSION OF 2′,7-BIS-MONOCHLOROACETYLPACLITAXEL ANALOGS TO 7-MONOCHLOROACETYL DERIVATIVES BY SOLVOLYSIS IN METHANOL. SYNTHETIC COMMUNICATIONS. 32:2711-2718.Full Text via DOI: 10.1081/scc-120006037
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2001Mechanistic considerations pertaining to the solvolysis of paclitaxel analogs bearing ester groups at the C2′ position. TETRAHEDRON LETTERS. 42:7747-7750.Full Text via DOI: 10.1016/s0040-4039(01)01643-4
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2000A Convenient Synthesis of 2-Phenylglycerol. SYNTHETIC COMMUNICATIONS. 30:4027-4038.Full Text via DOI: 10.1080/00397910008087018
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1997Utilization of a Benzoyl Migration To Effect an Expeditious Synthesis of the Paclitaxel C-13 Side Chain. ORGANIC PROCESS RESEARCH & DEVELOPMENT. 1:387-390.Full Text via DOI: 10.1021/op970113b
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1995Hydroxamic Acids as Potent Inhibitors of Endothelin-Converting Enzyme from Human Bronchiolar Smooth Muscle. JOURNAL OF MEDICINAL CHEMISTRY. 38:2119-2129.Full Text via DOI: 10.1021/jm00012a011
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1993(Imidazolylphenyl)pyrrol-2-one inhibitors of cardiac cAMP phosphodiesterase. JOURNAL OF MEDICINAL CHEMISTRY. 36:1041-1047.Full Text via DOI: 10.1021/jm00060a012
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1992Cardiotonic agents. 7. Prodrug derivatives of 4-ethyl-1,3-dihydro-5-[4-(2-methyl-1H-imidazol-1-yl)benzoyl]-2H-imidazol-2-one. JOURNAL OF MEDICINAL CHEMISTRY. 35:1267-1272.Full Text via DOI: 10.1021/jm00085a014
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1991Novel compounds possessing potent cAMP and cGMP phosphodiesterase inhibitory activity. Synthesis and cardiovascular effects of a series of imidazo[1,2-a]quinoxalinones and imidazo[1,5-a]quinoxalinones and their aza analogs. JOURNAL OF MEDICINAL CHEMISTRY. 34:2671-2677.Full Text via DOI: 10.1021/jm00113a002
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1991Synthesis and biological activity of angiotensin II analog containing a Val-His replacement, Val.psi.[CH(CONH2)HN]His. JOURNAL OF MEDICINAL CHEMISTRY. 34:2402-2410.Full Text via DOI: 10.1021/jm00112a014
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1990Cardiotonic agents. 6. Histamine analogs as potential cardiovascular selective H2 agonists. JOURNAL OF MEDICINAL CHEMISTRY. 33:1688-1697.Full Text via DOI: 10.1021/jm00168a024
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1989Cardiotonic agents. 5. Fragments from the heterocycle-phenyl-imidazole pharmacophore. JOURNAL OF MEDICINAL CHEMISTRY. 32:1173-1176.Full Text via DOI: 10.1021/jm00126a005
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1989Heterocyclic analogs of benzamide antiarrhythmic agents. JOURNAL OF MEDICINAL CHEMISTRY. 32:688-693.Full Text via DOI: 10.1021/jm00123a033
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1988Theoretical investigations of methanesulphonamide as a hydroxy group equivalent in drugs. Examples from possible β-adrenergic agents and analysis of computational methods. J. Chem. Soc., Perkin Trans. 2. 437-442.Full Text via DOI: 10.1039/p29880000437
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1987Cardiotonic agents. 1. Novel 8-aryl substituted imidazo[1,2-a]- and -[1,5-a]pyridines and imidazo[1,5-a]pyridinones as potential positive inotropic agents. JOURNAL OF MEDICINAL CHEMISTRY. 30:1337-1342.Full Text via DOI: 10.1021/jm00391a012
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1987Cardiotonic agents. 2. (Imidazolyl)aroylimidazolones, highly potent and selective positive inotropic agents. JOURNAL OF MEDICINAL CHEMISTRY. 30:1342-1347.Full Text via DOI: 10.1021/jm00391a013
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1987Facile Formation of Quaternary Azetidinium Compounds During Triflation of Dialkylaminopropanols. SYNTHETIC COMMUNICATIONS. 17:469-475.Full Text via DOI: 10.1080/00397918708063926
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1987In search of the digitalis replacement. JOURNAL OF MEDICINAL CHEMISTRY. 30:231-237.Full Text via DOI: 10.1021/jm00385a001
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1987β-Methylsulfonylamino phenethylamines and aryloxypropylamines as potential β-adrenergic agents. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. 22:165-167.Full Text via DOI: 10.1016/0223-5234(87)90014-6
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1983Benzylamine and Dibenzylamine Revisited. Syntheses of N-Substituted Aryloxypropanolamines Exemplifying a General Route to Secondary Aliphatic Amines. SYNTHETIC COMMUNICATIONS. 13:103-114.Full Text via DOI: 10.1080/00397918308061967
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1983Ultra-short-acting .beta.-adrenergic receptor blocking agents. 3. Ethylenediamine derivatives of (aryloxy)propanolamines having esters on the aryl function. JOURNAL OF MEDICINAL CHEMISTRY. 26:1109-1112.Full Text via DOI: 10.1021/jm00362a004
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1982Ultra-short acting beta-blockers: A proposal for the treatment of the critically ill patient. LIFE SCIENCES. 31:899-907.Full Text via DOI: 10.1016/0024-3205(82)90547-1
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1982Ultra-short-acting .beta.-adrenergic receptor blocking agents. 1. (Aryloxy)propanolamines containing esters in the nitrogen substituent. JOURNAL OF MEDICINAL CHEMISTRY. 25:1402-1407.Full Text via DOI: 10.1021/jm00354a002
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1982Ultra-short-acting .beta.-adrenergic receptor blocking agents. 2. (Aryloxy)propanolamines containing esters on the aryl function. JOURNAL OF MEDICINAL CHEMISTRY. 25:1408-1412.Full Text via DOI: 10.1021/jm00354a003
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1980Topographical Model of the Renal Vascular Dopamine Receptor. JOURNAL OF PHARMACEUTICAL SCIENCES. 69:1059-1061.Full Text via DOI: 10.1002/jps.2600690919
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Book Chapter (Web of Science)
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2013Glossary of Terms Used in Medicinal Chemistry Part II (IUPAC Recommendations 2013). ANNUAL REPORTS IN MEDICINAL CHEMISTRY, VOL 48. 387-418.Full Text via DOI: 10.1016/B978-0-12-417150-3.00024-7
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Correction (Web of Science)
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2017Correction: Corrigendum: Leukocyte integrin Mac-1 regulates thrombosis via interaction with platelet GPIbα. NATURE COMMUNICATIONS. 16124.Full Text via DOI: 10.1038/ncomms16124
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2003Corrigendum to “Mechanistic considerations pertaining to the solvolysis of paclitaxel analogs bearing ester groups at the C2′ position”. TETRAHEDRON LETTERS. 1985.Full Text via DOI: 10.1016/s0040-4039(03)00106-0
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1987Additions and Corrections - In Search of the Digitalis Replacement. JOURNAL OF MEDICINAL CHEMISTRY. 1938-1938.Full Text via DOI: 10.1021/jm00393a600
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Editorial Material (Web of Science)
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2000Medicinal chemistry in the development of societies. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. 1121-1125.Full Text via DOI: 10.1016/s0223-5234(00)01196-x
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Meeting Abstract (Web of Science)
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2016Translating molecular biology and clinical concepts into useful therapeutic agents within an academic-based drug discovery and development center: Importance of practical business considerations and extramural collaborations as well as meritorious technologies. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY.
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2013Design and development of glyceollin derived anti-cancer agents. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY.
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2013Indole-based chalcones as inducers of Methuosis. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY.
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2013Synthesis of soy phytoalexins having anti-cancer properties. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY.
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2012Design, synthesis, and biological evaluation of new species-selective inhibitors of aspartate semialdehyde dehydrogenase. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY.
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2011Molecular docking and 3D-QSAR studies for design and development of selective aspartate semialdehyde dehydrogenase inhibitors. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY.
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2011Synthesis and structure-activity relationships of compounds that induce methuosis, a novel type of non-apoptotic cell death. CANCER RESEARCH.Full Text via DOI: 10.1158/1538-7445.AM2011-666
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2010Synthetic scale-up and process optimization of glyceollin I, a novel natural product that displays interesting anticancer activity. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY.
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2010Total synthesis of racemic and natural glyceollin II. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY.
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2009ORGN 266-Ultrasound imaging for breast cancer. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY.
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2005Glyceollins (I-III), novel anti-estrogenic phytochemicals isolated from soy. BREAST CANCER RESEARCH AND TREATMENT. S202-S202.
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Note (Web of Science)
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1988Cardiotonic agents 4. Dimaprit analogues as potential cardiovascular selective H2-agonists. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. 295-300.Full Text via DOI: 10.1016/0223-5234(88)90013-x
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1980Analysis of procainamide hydrochloride and acecainide hydrochloride in rat feed. JOURNAL OF PHARMACEUTICAL SCIENCES. 1439-1440.Full Text via DOI: 10.1002/jps.2600691224
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Patent (Faculty180)
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Review Article (Web of Science)
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2013Glossary of Terms Used in Medicinal Chemistry Part II (IUPAC Recommendations 2013). Annual Reports in Medicinal Chemistry. 387-418.Full Text via DOI: 10.1016/b978-0-12-417150-3.00024-7
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2003A Human Drug Metabolism Database: Potential Roles in the Quantitative Predictions of Drug Metabolism and Metabolism-Related Drug-Drug Interactions. CURRENT DRUG METABOLISM. 411-422.Full Text via DOI: 10.2174/1389200033489299
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2002Medicinal chemistry in the new millennium. A glance into the future. PURE AND APPLIED CHEMISTRY. 703-785.Full Text via DOI: 10.1351/pac200274050703
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1991A topographical model for the c-AMP phosphodiesterase III active site. LIFE SCIENCES. 553-568.Full Text via DOI: 10.1016/0024-3205(91)90254-9
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