D. Karanewsky

发表

The sweet taste of true synergy: positive allosteric modulation of the human sweet taste receptor.

Xiaodong Li, G. Servant, C. Tachdjian, 2011, Trends in pharmacological sciences.

Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists.

M. Faul, L. L. Winneroski, C. Broderick, 2001, Journal of medicinal chemistry.

Design and synthesis of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 1.

Jennifer L. Harris, R. Epple, B. Bursulaya, 2005, Bioorganic & medicinal chemistry letters.

Discovery of GNF-5837, a Selective TRK Inhibitor with Efficacy in Rodent Cancer Tumor Models.

Nanxin Li, A. Kreusch, Shenlin Huang, 2012, ACS medicinal chemistry letters.

Conformationally constrained inhibitors of caspase-1 (interleukin-1 beta converting enzyme) and of the human CED-3 homologue caspase-3 (CPP32, apopain).

K. Tomaselli, J. Krebs, J. Wu, 1998, Bioorganic & medicinal chemistry letters.

The ClpP activator ONC‐212 (TR‐31) inhibits BCL2 and B‐cell receptor signaling in CLL

E. Iwanowicz, R. Christopherson, O. G. Best, 2021, EJHaem.

Novel (2E,4E,6Z)-7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta-2,4,6-trienoic acid retinoid X receptor modulators are active in models of type 2 diabetes.

M. D. Leibowitz, M. Faul, M. Boehm, 2003, Journal of medicinal chemistry.

Design and synthesis of novel RXR-selective modulators with improved pharmacological profile.

M. D. Leibowitz, M. Boehm, T. Grese, 2003, Bioorganic & medicinal chemistry letters.

Mitochondrial Protease ClpP is a Target for the Anticancer Compounds ONC201 and Related Analogues

Laura E. Herring, E. Iwanowicz, P. Graves, 2019, ACS chemical biology.

Structure-activity relationships within a series of caspase inhibitors: effect of leaving group modifications.

J. Díaz, A. Schmitz, T. Deckwerth, 2003, Bioorganic & medicinal chemistry letters.

Potent, nonsteroidal selective androgen receptor modulators (SARMs) based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones.

J. Edwards, E. Kallel, D. Karanewsky, 2007, Bioorganic & medicinal chemistry letters.

The CIpP activator, TR-57, is highly effective as a single agent and in combination with venetoclax against CLL cells in vitro

E. Iwanowicz, R. Christopherson, O. G. Best, 2022, bioRxiv.

First-in-class pan caspase inhibitor developed for the treatment of liver disease.

N. Chen, J. Díaz, K. Valentino, 2005, Journal of medicinal chemistry.

Characterization of the caspase inhibitor IDN-1965 in a model of apoptosis-associated liver injury.

K. Valentino, K. Tomaselli, A. Srinivasan, 2001, The Journal of pharmacology and experimental therapeutics.

Discovery of pyrimidine benzimidazoles as Lck inhibitors: part I.

N. Gray, Jianwei Che, P. Ren, 2008, Bioorganic & medicinal chemistry letters.

Discovery of nonsteroidal glucocorticoid receptor ligands based on 6-indole-1,2,3,4-tetrahydroquinolines.

Yan Liu, Steven L. Roach, J. Miner, 2008, Bioorganic & medicinal chemistry letters.

Positive allosteric modulators of the human sweet taste receptor enhance sweet taste

Xiaodong Li, Mark Zoller, G. Servant, 2010, Proceedings of the National Academy of Sciences.

Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II.

N. Gray, Jianwei Che, P. Ren, 2009, Bioorganic & medicinal chemistry letters.

Discovery of 2-amino-6-carboxamidobenzothiazoles as potent Lck inhibitors.

Shenlin Huang, R. Romeo, M. Sandberg, 2008, Bioorganic & medicinal chemistry letters.

Oxamyl dipeptide caspase inhibitors developed for the treatment of stroke.

A. Sauter, J. Díaz, A. Schmitz, 2004, Bioorganic & medicinal chemistry letters.

Phosphorus-containing inhibitors of HMG-CoA reductase. 2. Synthesis and biological activities of a series of substituted pyridines containing a hydroxyphosphinyl moiety.

E. Gordon, J. Pluščec, T. Harrity, 1991, Journal of medicinal chemistry.

Toxicological evaluation and metabolism of two N-alkyl benzamide umami flavour compounds: N-(heptan-4-yl)benzo[d][1,3]dioxole-5-carboxamide and (R)-N-(1-methoxy-4-methylpentan-2-yl)-3,4-dimethylbenzamide

D. Karanewsky, Hanghui Liu, A. Arthur, 2016, Toxicology reports.

Toxicological evaluation of a novel umami flavour compound: 2-(((3-(2,3-Dimethoxyphenyl)-1H-1,2,4-triazol-5-yl)thio)methyl)pyridine

S. Markison, D. Karanewsky, Hanghui Liu, 2016, Toxicology reports.

Selective androgen receptor modulators based on a series of 7H-[1,4]oxazino[3,2-g]quinolin-7-ones with improved in vivo activity.

Min Wu, William Y. Chang, D. Karanewsky, 2008, Bioorganic & medicinal chemistry letters.

Toxicological evaluation of the flavour ingredient N-(1-((4-amino-2,2-dioxido-1H-benzo[c][1,2,6]thiadiazin-5-yl)oxy)-2-methylpropan-2-yl)-2,6-dimethylisonicotinamide (S2218)

G. Servant, C. Tachdjian, D. Karanewsky, 2017, Toxicology reports.

Toxicological evaluation of the flavour ingredient 4-amino-5-(3-(isopropylamino)-2,2-dimethyl-3-oxopropoxy)-2-methylquinoline-3-carboxylic acid

S. Markison, D. Karanewsky, Hanghui Liu, 2015, Toxicology reports.

Toxicological evaluation of two flavors with modifying properties: 3-((4-amino-2,2-dioxido-1H-benzo[c][1,2,6]thiadiazin-5-yl)oxy)-2,2-dimethyl-N-propylpropanamide and (S)-1-(3-(((4-amino-2,2-dioxido-1H-benzo[c][1,2,6]thiadiazin-5-yl)oxy)methyl)piperidin-1-yl)-3-methylbutan-1-one.

D. Karanewsky, G. Goodfellow, A. Arthur, 2015, Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association.

Potent ClpP agonists with anticancer properties bind with improved structural complementarity and alter the mitochondrial N-terminome.

A. Gingras, W. Houry, E. Iwanowicz, 2022, Structure.

DUAL METALLOPROTEASE INHIBITORS. IV: UTILIZATION OF THIAZEPINES AND THIAZINES AS CONSTRAINED PEPTIDOMIMETIC SURROGATES IN MERCAPTOACYL DIPEPTIDES

N. Trippodo, R. Misra, J. Das, 1994 .

Dual metalloprotease inhibitors. I. constrained peptidomimetics of mercaptoacyl dipeptides

J. Barrish, N. Murugesan, N. Trippodo, 1994 .

Novel bisaryl substituted thiazoles and oxazoles as highly potent and selective peroxisome proliferator-activated receptor delta agonists.

J. Wityak, E. Saez, R. Epple, 2010, Journal of medicinal chemistry.

Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.

J. Caldwell, K. Kuhen, B. Bursulaya, 2006, Bioorganic & medicinal chemistry letters.

An efficient and mild synthesis of highly substituted imidazoles

J. Stafford, M. Brackeen, P. Feldman, 1994 .

Optimization of small molecule agonists of the thrombopoietin (Tpo) receptor derived from a benzo[a]carbazole hit scaffold.

J. Lao, D. Chow, T. Marsilje, 2008, Bioorganic & medicinal chemistry letters.

Synthesis and evaluation of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 3: heterocyclic P3.

Jun Li, Glen Spraggon, Tove Tuntland, 2006, Bioorganic & medicinal chemistry letters.

Discovery and biological evaluation of benzo[a]carbazole-based small molecule agonists of the thrombopoietin (Tpo) receptor.

J. Lao, A. Chatterjee, T. Tuntland, 2008, Bioorganic & medicinal chemistry letters.

A highly selective protocol for the deprotection of BOC-protected amides and carbamates

J. Stafford, M. Brackeen, D. Karanewsky, 1993 .

Vasopeptidase inhibitors: incorporation of geminal and spirocyclic substituted azepinones in mercaptoacyl dipeptides.

N. Trippodo, E. Sieber-McMaster, J. Robl, 1999, Journal of medicinal chemistry.

(Phosphinyloxy)acyl amino acid inhibitors of angiotensin converting enzyme (ACE). 1. Discovery of (S)-1-[6-amino-2-[[hydroxy(4-phenylbutyl)phosphinyl]oxy]-1-oxohexyl]-L -proline a novel orally active inhibitor of ACE.

D W Cushman, D. W. Cushman, J. M. Deforrest, 1988, Journal of medicinal chemistry.

(Phosphinyloxy)acyl amino acid inhibitors of angiotensin converting enzyme. 2. Terminal amino acid analogues of (S)-1-[6-amino-2 [[hydroxy(4-phenylbutyl)phosphinyl]oxy]-1-oxohexyl]-L-proline.

D W Cushman, V. Lee, D. W. Cushman, 1990, Journal of medicinal chemistry.

Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.

J. Caldwell, K. Kuhen, B. Bursulaya, 2006, Bioorganic & medicinal chemistry letters.

SYNTHETIC STUDIES ON POLYETHER ANTIBIOTICS. 6. TOTAL SYNTHESIS OF MONENSIN. 3. STEREOCONTROLLED TOTAL SYNTHESIS OF MONENSIN

T. Fukuyama, Y. Kishi, G. Schmid, 2002 .

Practical synthesis of an enantiomerically pure synthon for the preparation of mevinic acid analogs

D. Karanewsky, M. Malley, J. Gougoutas, 1991 .

Synthesis of phosphonic monoesters from phosphonous acids

D. Karanewsky, M. Badia, 1986 .

Preparation of optically active 2-aminoalkylphosphinic and phosphonic acids

M. Duggan, D. Karanewsky, 1983 .

Phosphorus-containing inhibitors of HMG-CoA reductase. 1. 4-[(2-arylethyl)hydroxyphosphinyl]-3-hydroxy-butanoic acids: a new class of cell-selective inhibitors of cholesterol biosynthesis.

E. Gordon, T. Harrity, M. Sofia, 1990, Journal of medicinal chemistry.

New conditions for controlled Claisen rearrangements of allyl aryl ethers

Y. Kishi, D. Karanewsky, 1976 .

SYNTHESIS OF BENZO-FUSED, 7,5- AND 7,6-FUSED AZEPINONES AS CONFORMATIONALLY RESTRICTED DIPEPTIDE MIMETICS

J. Robl, D. Karanewsky, M. Asaad, 1995 .

Design, synthesis, and structure-activity relationship studies of novel 6,7-locked-[7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta]-2,4,6-trienoic acids.

M. D. Leibowitz, C. Montrose‐Rafizadeh, M. Boehm, 2003, Journal of medicinal chemistry.

Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.

J. Caldwell, K. Kuhen, H. Yin, 2006, Bioorganic & medicinal chemistry letters.

Structure-activity relationships within a series of caspase inhibitors. Part 2: Heterocyclic warheads.

N. Chen, J. Díaz, A. Schmitz, 2005, Bioorganic & medicinal chemistry letters.

5(Z)-benzylidene-1,2-dihydro-9-hydroxy-10-methoxy-2,2,4-trimethyl-5H-1-aza-6-oxa-chrysenes as non-steroidal glucocorticoid receptor modulators.

Steven L. Roach, J. Miner, A. Negro-Vilar, 2007, Bioorganic & Medicinal Chemistry Letters.

Structure—Activity Relationships and Sub‐Type Selectivity in an Oxabicyclic Estrogen Receptor α/β Agonist Scaffold.

L. Hamann, D. Karanewsky, E. Allegretto, 2005 .

Structure–activity relationships and sub-type selectivity in an oxabicyclic estrogen receptor α/β agonist scaffold

L. Hamann, D. Karanewsky, E. Allegretto, 2005 .

Synthetic transformations of the mevinic acid nucleus: Preparation of a monocyclic analogue of compactin

D. Karanewsky, 1991 .

Phosphorus-containing inhibitors of HMG-CoA Reductase. 3. Synthesis of hydroxyphosphinyl-analogues of the mevinic acids

D. Karanewsky, M. Badia, 1993 .

Phosphorus‐Containing Inhibitors of HMG‐CoA Reductase. Part 3. Synthesis of Hydroxyphosphinyl Analogues of the Mevinic Acids.

D. Karanewsky, M. Badia, 1993 .

Angiotensin-converting enzyme inhibitors. Mercaptan, carboxyalkyl dipeptide, and phosphinic acid inhibitors incorporating 4-substituted prolines.

D W Cushman, D. W. Cushman, J. M. Deforrest, 1988, Journal of medicinal chemistry.

Toxicological evaluation of two novel bitter modifying flavour compounds: 3-(1-((3,5-dimethylisoxazol-4-yl)methyl)-1H-pyrazol-4-yl)-1-(3-hydroxybenzyl)imidazolidine-2,4-dione and 3-(1-((3,5-dimethylisoxazol-4-yl)methyl)-1H-pyrazol-4-yl)-1-(3-hydroxybenzyl)-5,5-dimethylimidazolidine-2,4-dione

S. Markison, D. Karanewsky, Hanghui Liu, 2016, Toxicology reports.

Pharmacology of caspase inhibitors in rabbit cardiomyocytes subjected to metabolic inhibition and recovery.

K. Valentino, R. Gottlieb, R. Engler, 2001, Antioxidants & redox signaling.

Activation of the CED3/ICE-Related Protease CPP32 in Cerebellar Granule Neurons Undergoing Apoptosis But Not Necrosis

E. Alnemri, R. Armstrong, L. Fritz, 1997, The Journal of Neuroscience.

Activation of Membrane-associated Procaspase-3 Is Regulated by Bcl-2

A. Schmitz, R. Armstrong, L. Fritz, 1999, The Journal of cell biology.

Discovery and Development of S6821 and S7958 as Potent TAS2R8 Antagonists.

G. Servant, Lan Zhang, Tanya L. Ditschun, 2020, Journal of medicinal chemistry.

Fas-induced Activation of the Cell Death-related Protease CPP32 Is Inhibited by Bcl-2 and by ICE Family Protease Inhibitors*

S. Korsmeyer, J. Xiang, R. Armstrong, 1996, The Journal of Biological Chemistry.

Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 2.

J. Caldwell, N. Gray, T. Honda, 2006, Bioorganic & medicinal chemistry letters.

Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 1.

J. Caldwell, N. Gray, O. Ohmori, 2006, Bioorganic & medicinal chemistry letters.

Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2

Sungjoon Kim, Nanxin Li, M. Warmuth, 2013, Journal of medicinal chemistry.

Structure of Recombinant Human CPP32 in Complex with the Tetrapeptide Acetyl-Asp-Val-Ala-Asp Fluoromethyl Ketone*

M. Grütter, P. Mittl, J. Priestle, 1997, The Journal of Biological Chemistry.

Characterization of TR‐107, a novel chemical activator of the human mitochondrial protease ClpP

W. Houry, E. Iwanowicz, C. Der, 2022, bioRxiv.

DUAL METALLOPROTEASE INHIBITORS. III: UTILIZATION OF BICYCLIC AND MONOCYCLIC DIAZEPINONE BASED MERCAPTOACETYLS

J. Barrish, N. Trippodo, J. Robl, 1994 .

Dual metalloprotease inhibitors. II. Effect of substitution and stereochemistry on benzazepinone based mercaptoacetyls

N. Trippodo, R. Misra, E. Sieber-McMaster, 1994 .

Rational Design and Biochemical Utility of Specific Inhibitors of Angiotensin‐Converting Enzyme

E. Gordon, S. Natarajan, M. Ondetti, 1987, Journal of cardiovascular pharmacology.

Phosphorus-Containing Inhibitors of HMG-CoA Reductase. Part 1. 4-((2- Arylethyl)hydroxyphosphinyl)-3-hydroxybutanoic Acids: A New Class of Cell-Selective Inhibitors of Cholesterol Biosynthesis.

E. Gordon, T. Harrity, M. Sofia, 1991 .

Acyl dipeptides as reversible caspase inhibitors. Part 2: further optimization.

N. Chen, J. Díaz, A. Schmitz, 2002, Bioorganic & medicinal chemistry letters.

Acyl dipeptides as reversible caspase inhibitors. Part 1: initial lead optimization.

J. Díaz, L. Fritz, K. Tomaselli, 2002, Bioorganic & medicinal chemistry letters.

Design, synthesis and structure-activity relationship of novel RXR-selective modulators.

M. D. Leibowitz, M. Boehm, T. Grese, 2004, Bioorganic & medicinal chemistry letters.

3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists. Part 2.

J. Wityak, A. Kreusch, E. Saez, 2006, Bioorganic & medicinal chemistry letters.

Androstene-17-thioketals. 2nd communication: pharmacological profiles of tipredane and (11 beta, 17 alpha)-17-(ethylthio)-9 alpha-fluoro-17-[2-(fluoroethyl)thio]-11 beta-hydroxy-androsta-1,4-dien-3-one, structurally novel 20-thiasteroids possessing potent and selective topical antiinflammatory activ

C. Free, D. Karanewsky, R. Varma, 1986, Arzneimittel-Forschung.

Synthesis and SAR of arylaminoethyl amides as noncovalent inhibitors of cathepsin S: P3 cyclic ethers.

Jun Li, Glen Spraggon, Tove Tuntland, 2006, Bioorganic & medicinal chemistry letters.

Arylaminoethyl carbamates as a novel series of potent and selective cathepsin S inhibitors.

Jun Li, Tove Tuntland, Jennifer L. Harris, 2006, Bioorganic & medicinal chemistry letters.

Arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 2: Optimization of P1 and N-aryl.

Jennifer L. Harris, A. Chatterjee, T. Hollenbeck, 2006, Bioorganic & Medicinal Chemistry Letters.

Toxicological evaluation of a novel cooling compound: 2-(4-methylphenoxy)-N-(1H-pyrazol-3-yl)-N-(2-thienylmethyl)acetamide

S. Markison, D. Karanewsky, Hanghui Liu, 2015, Toxicology reports.

Discovery of 2-amino-6-carboxamidobenzothiazoles as potent Lck inhibitors.

Shenlin Huang, R. Romeo, T. Spalding, 2008, Bioorganic & medicinal chemistry letters.