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1

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

David Ellis, Kelli L. Kuhen, Beth Anaclerio, Baogen Wu, Karen Wolff, Hong Yin, Badry Bursulaya, Jeremy Caldwell, Donald Karanewsky, Yun He

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2006

Langue:

english

Fichier:

PDF, 153 KB

english, 2006

2

Design, Synthesis and Structure—Activity Relationship of Novel RXR-Selective Modulators.

Pierre-Yves Michellys, Jennifer D'Arrigo, Timothy A. Grese, Donald S. Karanewsky, Mark D. Leibowitz, Dale A. Mais, Christopher M. Mapes, Anne Reifel-Miller, Deepa Rungta, Marcus F. Boehm

Journal:

Année:

2004

Fichier:

PDF, 183 KB

2004

3

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

Lawrence G. Hamann, J. Hoyt Meyer, Daniel A. Ruppar, Keith B. Marschke, Francisco J. Lopez, Elizabeth A. Allegretto, Donald S. Karanewsky

Journal:

Année:

2005

Fichier:

PDF, 16 KB

2005

4

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

Donald S. Karanewsky

Journal:

Tetrahedron Letters

Année:

1991

Langue:

english

Fichier:

PDF, 272 KB

english, 1991

5

An efficient and mild synthesis of highly substituted imidazoles

Marcus F. Brackeen, Jeffrey A. Stafford, Paul L. Feldman, Donald S. Karanewsky

Journal:

Tetrahedron Letters

Année:

1994

Langue:

english

Fichier:

PDF, 259 KB

english, 1994

6

Synthesis of benzo-fused, 7,5- and 7,6-fused azepinones as conformationally restricted dipeptide mimetics

Jeffrey A. Robl, Donald S. Karanewsky, Magdi M. Asaad

Journal:

Tetrahedron Letters

Année:

1995

Langue:

english

Fichier:

PDF, 246 KB

english, 1995

7

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

Steven L. Roach, Robert I. Higuchi, Mark E. Adams, Yan Liu, Donald S. Karanewsky, Keith B. Marschke, Dale E. Mais, Jeffrey N. Miner, Lin Zhi

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2008

Langue:

english

Fichier:

PDF, 200 KB

english, 2008

8

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

Pierre-Yves Michellys, Marcus F Boehm, Jyun-Hung Chen, Timothy A Grese, Donald S Karanewsky, Mark D Leibowitz, Sha Liu, Dale A Mais, Christopher M Mapes, Anne Reifel-Miller, Katheen M Ogilvie, Deepa R

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2003

Langue:

english

Fichier:

PDF, 239 KB

english, 2003

9

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

Lawrence G. Hamann, J. Hoyt Meyer, Daniel A. Ruppar, Keith B. Marschke, Francisco J. Lopez, Elizabeth A. Allegretto, Donald S. Karanewsky

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2005

Langue:

english

Fichier:

PDF, 144 KB

english, 2005

10

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

Brett R. Ullman, Teresa Aja, Ning Chen, Jose-Luis Diaz, Xin Gu, Julia Herrmann, Vincent J. Kalish, Donald S. Karanewsky, Lalitha Kodandapani, Joseph J. Krebs, Steven D. Linton, Steven P. Meduna, Kip N

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2005

Langue:

english

Fichier:

PDF, 184 KB

english, 2005

11

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

Ha-Soon Choi, Zhicheng Wang, Wendy Richmond, Xiaohui He, Kunyong Yang, Tao Jiang, Taebo Sim, Donald Karanewsky, Xiang-ju Gu, Vicki Zhou, Yi Liu, Osamu Ohmori, Jeremy Caldwell, Nathanael Gray, Yun He

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2006

Langue:

english

Fichier:

PDF, 138 KB

english, 2006

12

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

Ha-Soon Choi, Zhicheng Wang, Wendy Richmond, Xiaohui He, Kunyong Yang, Tao Jiang, Donald Karanewsky, Xiang-ju Gu, Vicki Zhou, Yi Liu, Jianwei Che, Christian C. Lee, Jeremy Caldwell, Takanori Kanazawa,

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2006

Langue:

english

Fichier:

PDF, 275 KB

english, 2006

13

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

Baogen Wu, Kelli Kuhen, Truc Ngoc Nguyen, David Ellis, Beth Anaclerio, Xiaohui He, Kunyong Yang, Donald Karanewsky, Hong Yin, Karen Wolff, Kimberly Bieza, Jeremy Caldwell, Yun He

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2006

Langue:

english

Fichier:

PDF, 120 KB

english, 2006

14

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

Shenlin Huang, Zuosheng Liu, Shin-Shay Tian, Mark Sandberg, Tracy A. Spalding, Russell Romeo, Maya Iskandar, Zhiliang Wang, Donald Karanewsky, Yun He

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2008

Langue:

english

Fichier:

PDF, 130 KB

english, 2008

15

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

Phil B. Alper, Thomas H. Marsilje, Daniel Mutnick, Wenshuo Lu, Arnab Chatterjee, Michael J. Roberts, Yun He, Donald S. Karanewsky, Donald Chow, Jianmin Lao, Andrea Gerken, Tove Tuntland, Bo Liu, Jonat

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2008

Langue:

english

Fichier:

PDF, 196 KB

english, 2008

16

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

Thomas H. Marsilje, Phil B. Alper, Wenshuo Lu, Daniel Mutnick, Pierre-Yves Michellys, Yun He, Donald S. Karanewsky, Donald Chow, Andrea Gerken, Jianmin Lao, Min-Ju Kim, H. Martin Seidel, Shin-Shay Tia

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2008

Langue:

english

Fichier:

PDF, 225 KB

english, 2008

17

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

Donald S. Karanewsky, Michael C. Badia

Journal:

Tetrahedron Letters

Année:

1993

Langue:

english

Fichier:

PDF, 284 KB

english, 1993

18

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

Jeffrey A. Stafford, Marcus F. Brackeen, Donald S. Karanewsky, Nicole L. Valvano

Journal:

Tetrahedron Letters

Année:

1993

Langue:

english

Fichier:

PDF, 271 KB

english, 1993

19

Synthesis of phosphonic monoesters from phosphonous acids

Donald S Karanewsky, Michael C Badia

Journal:

Tetrahedron Letters

Année:

1986

Langue:

english

Fichier:

PDF, 251 KB

english, 1986

20

Preparation of optically active 2-aminoalkylphosphinic and phosphonic acids

Mark E. Duggan, Donald S. Karanewsky

Journal:

Tetrahedron Letters

Année:

1983

Langue:

english

Fichier:

PDF, 192 KB

english, 1983

21

Dual metalloprotease inhibitors. III. utilization of bicyclic and monocyclic diazepinone based mercaptoacetyls

Jeffrey A. Robl, Chong-Qing Sun, Ligaya M. Simpkins, Denis E. Ryono, Joel C. Barrish, Donald S. Karanewsky, Magdi M. Asaad, Thomas R. Schaeffer, Nick C. Trippodo

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

1994

Langue:

english

Fichier:

PDF, 505 KB

english, 1994

22

Acyl dipeptides as reversible caspase inhibitors. Part 1: Initial Lead Optimization

Steven D. Linton, Donald S. Karanewsky, Robert J. Ternansky, Joe C. Wu, Brian Pham, Lalitha Kodandapani, Robert Smidt, Jose-Luis Diaz, Lawrence C. Fritz, Kevin J. Tomaselli

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2002

Langue:

english

Fichier:

PDF, 106 KB

english, 2002

23

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

Steven D. Linton, Donald S. Karanewsky, Robert J. Ternansky, Ning Chen, Xian Guo, Kathy G. Jahangiri, Vincent J. Kalish, Steven P. Meduna, Edward D. Robinson, Brett R. Ullman, Joe C. Wu, Brian Pham, L

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2002

Langue:

english

Fichier:

PDF, 99 KB

english, 2002

24

Structure–Activity relationships within a series of caspase inhibitors: effect of leaving group modifications

Brett R. Ullman, Teresa Aja, Thomas L. Deckwerth, Jose-Luis Diaz, Julia Herrmann, Vincent J. Kalish, Donald S. Karanewsky, Steven P. Meduna, Kip Nalley, Edward D. Robinson, Silvio P. Roggo, Robert O.

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2003

Langue:

english

Fichier:

PDF, 178 KB

english, 2003

25

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

Donald S. Karanewsky, Xu Bai, Steven D. Linton, Joseph F. Krebs, Joe Wu, Bryan Pham, Kevin J. Tomaselli

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

1998

Langue:

english

Fichier:

PDF, 351 KB

english, 1998

26

Oxamyl dipeptide caspase inhibitors developed for the treatment of stroke

Steven D. Linton, Teresa Aja, Peter R. Allegrini, Thomas L. Deckwerth, Jose-Luis Diaz, Bastian Hengerer, Julia Herrmann, Kathy G. Jahangiri, Joerg Kallen, Donald S. Karanewsky, Steven P. Meduna, Kip N

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2004

Langue:

english

Fichier:

PDF, 295 KB

english, 2004

27

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

Pierre-Yves Michellys, Jennifer D'Arrigo, Timothy A. Grese, Donald S. Karanewsky, Mark D. Leibowitz, Dale A. Mais, Christopher M. Mapes, Anne Reifel-Miller, Deepa Rungta, Marcus F. Boehm

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2004

Langue:

english

Fichier:

PDF, 255 KB

english, 2004

28

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

Tao Jiang, Kelli L. Kuhen, Karen Wolff, Hong Yin, Kimberly Bieza, Jeremy Caldwell, Badry Bursulaya, Tove Tuntland, Kanyin Zhang, Donald Karanewsky, Yun He

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2006

Langue:

english

Fichier:

PDF, 156 KB

english, 2006

29

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

Krapcho, John, Turk, Chester, Cushman, David W., Powell, James R., DeForrest, Jack M., Spitzmiller, Ervin R., Karanewsky, Donald S., Duggan, Mark, Rovnyak, George

Journal:

Journal of Medicinal Chemistry

Année:

1988

Langue:

english

Fichier:

PDF, 2.47 MB

english, 1988

30

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

Guy Servant, Catherine Tachdjian, Xiaodong Li, Donald S. Karanewsky

Journal:

Trends in Pharmacological Sciences

Année:

2011

Langue:

english

Fichier:

PDF, 687 KB

english, 2011

31

(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

Karanewsky, Donald S., Badia, Michael C., Cushman, David W., DeForrest, Jack M., Dejneka, Tamara, Loots, Melanie J., Perri, Maria G., Petrillo, Edward W., Powell, James R.

Journal:

Journal of Medicinal Chemistry

Année:

1988

Langue:

english

Fichier:

PDF, 1.25 MB

english, 1988

32

Design and Synthesis of 2-Methyl-2-{4-[2-(5-methyl-2-aryloxazol- 4-yl)ethoxy]phenoxy}propionic Acids: A New Class of Dual PPARα/γ Agonists

Brooks, Dawn A., Etgen, Garret J., Rito, Christopher J., Shuker, Anthony J., Dominianni, Samuel J., Warshawsky, Alan M., Ardecky, Robert, Paterniti, James R., Tyhonas, John, Karanewsky, Donald S., Kau

Journal:

Journal of Medicinal Chemistry

Année:

2001

Langue:

english

Fichier:

PDF, 63 KB

english, 2001

33

Novel Bisaryl Substituted Thiazoles and Oxazoles as Highly Potent and Selective Peroxisome Proliferator-Activated Receptor δ Agonists

Epple, Robert, Cow, Christopher, Xie, Yongping, Azimioara, Mihai, Russo, Ross, Wang, Xing, Wityak, John, Karanewsky, Donald S., Tuntland, Tove, Nguyêñ-Trân, Vân T. B., Cuc Ngo, Cara, Huang, David,

Journal:

Journal of Medicinal Chemistry

Année:

2010

Langue:

english

Fichier:

PDF, 1.63 MB

english, 2010

34

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

Michellys, Pierre-Yves, Ardecky, Robert J., Chen, Jyun-Hung, D'Arrigo, Jennifer, Grese, Timothy A., Karanewsky, Donald S., Leibowitz, Mark D., Liu, Sha, Mais, Dale A., Mapes, Christopher M., Montrose-

Journal:

Journal of Medicinal Chemistry

Année:

2003

Langue:

english

Fichier:

PDF, 236 KB

english, 2003

35

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

Karanewsky, Donald S., Badia, Michael C., Cushman, David W., DeForrest, Jack M., Dejneka, Tamara, Lee, Ving G., Loots, Melanie J., Petrillo, Edward W.

Journal:

Journal of Medicinal Chemistry

Année:

1990

Langue:

english

Fichier:

PDF, 1.49 MB

english, 1990

36

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

Joseph F. Krebs, Robert C. Armstrong, Anu Srinivasan, Teresa Aja, Angela M. Wong, Aileen Aboy, Rob Sayers, Bryan Pham, Tam Vu, Kim Hoang, Donald S. Karanewsky, Christian Leist, Albert Schmitz, Joe C.

Journal:

The Journal of Cell Biology

Année:

1999

Langue:

english

Fichier:

PDF, 3.08 MB

english, 1999

37

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

Robl, Jeffrey A., Duncan, Laurelee A., Pluscec, Jelka, Karanewsky, Donald S., Gordon, Eric M., Ciosek, Carl P., Rich, Lois C., Dehmel, Viviane C., Slusarchyk, Dorothy A.

Journal:

Journal of Medicinal Chemistry

Année:

1991

Langue:

english

Fichier:

PDF, 1.72 MB

english, 1991

38

Phosphorus-containing inhibitors of HMG-CoA reductase. I. 4-[(2-Arylethyl)hydroxyphosphinyl]-3-hydroxybutanoic acids: a new class of cell selective inhibitors of cholesterol biosynthesis

Karanewsky, Donald S., Badia, Michael C., Ciosek, Carl P., Robl, Jeffrey A., Sofia, Michael J., Simpkins, Ligaya M., DeLange, Barbara, Harrity, Thomas W., Biller, Scott A., Gordon, Eric M.

Journal:

Journal of Medicinal Chemistry

Année:

1990

Langue:

english

Fichier:

PDF, 615 KB

english, 1990

39

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

Karanewsky, Donald S., Malley, Mary F., Gougoutas, Jack Z.

Journal:

Journal of Organic Chemistry

Année:

1991

Langue:

english

Fichier:

PDF, 581 KB

english, 1991

40

Vasopeptidase Inhibitors: Incorporation of Geminal and Spirocyclic Substituted Azepinones in Mercaptoacyl Dipeptides

Robl, Jeffrey A., Sulsky, Richard, Sieber-McMaster, Ellen, Ryono, Denis E., Cimarusti, Maria P., Simpkins, Ligaya M., Karanewsky, Donald S., Chao, Sam, Asaad, Magdi M., Seymour, Andrea A., Fox, Maxine

Journal:

Journal of Medicinal Chemistry

Année:

1999

Langue:

english

Fichier:

PDF, 141 KB

english, 1999

41

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

Arthur, Amy J., Karanewsky, Donald S., Luksic, Mike, Goodfellow, Geoff, Daniels, Jon

Journal:

Food and Chemical Toxicology

Année:

2015

Langue:

english

Fichier:

PDF, 712 KB

english, 2015

42

Toxicological Evaluation of a Novel Cooling Compound: 2-(4-methylphenoxy)-N-(1H-pyrazol-3-yl)-N-(2-thienylmethyl)acetamide

Karanewsky, Donald S., Arthur, Amy J., Liu, Hanghui, Chi, Bert, Markison, Stacy

Journal:

Toxicology Reports

Année:

2015

Langue:

english

Fichier:

PDF, 1.00 MB

english, 2015

43

Toxicological Evaluation of a Novel Umami Flavour Compound: 2-(((3-(2,3-dimethoxyphenyl)-1H-1,2,4-triazol-5-yl)thio)methyl)pyridine

Karanewsky, Donald S., Arthur, Amy J., Liu, Hanghui, Chi, Bert, Ida, Lily, Markison, Stacy

Journal:

Toxicology Reports

Année:

2016

Langue:

english

Fichier:

PDF, 932 KB

english, 2016

44

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

Karanewsky, Donald S., Arthur, Amy J., Liu, Hanghui, Chi, Bert, Ida, Lily, Markison, Stacy

Journal:

Toxicology Reports

Année:

2016

Langue:

english

Fichier:

PDF, 1.36 MB

english, 2016

45

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

Arthur, Amy J., Karanewsky, Donald S., Liu, Hanghui, Chi, Bert, Markison, Stacy

Journal:

Toxicology Reports

Année:

2015

Langue:

english

Fichier:

PDF, 762 KB

english, 2015

46

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

Karanewsky, Donald S., Arthur, Amy J., Liu, Hanghui, Chi, Bert, Ida, Lily

Journal:

Toxicology Reports

Année:

2016

Langue:

english

Fichier:

PDF, 1.00 MB

english, 2016

47

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

Karanewsky, Donald S., Servant, Guy, Liu, Hanghui, Chi, Bert, Ida, Lily, Saganich, Michael, Werner, Sara, Fotsing, Joseph R., Patron, Andrew, Tachdjian, Catherine, Arthur, Amy

Journal:

Toxicology Reports

Année:

2017

Langue:

english

Fichier:

PDF, 693 KB

english, 2017

48

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

Armstrong, Robert C., Aja, Teresa J., Hoang, Kim D., Gaur, Smita, Bai, Xu, Alnemri, Emad S., Litwack, Gerald, Karanewsky, Donald S., Fritz, Lawrence C., Tomaselli, Kevin J.

Journal:

Journal of Neuroscience

Année:

1997

Langue:

english

Fichier:

PDF, 460 KB

english, 1997