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1

What is next for small-molecule drug discovery?

Doweyko, Arthur M, Doweyko, Lidia M

Journal:

Future Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 523 KB

english, 2009

2

Structural Comparison of p38 Inhibitor-Protein Complexes: A Review of Recent p38 Inhibitors Having Unique Binding Interactions

Wrobleski, Stephen, Doweyko, Arthur

Journal:

Current Topics in Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 318 KB

english, 2005

3

A New Class of High Affinity Thyromimetics Containing a Phenyl-naphthylene Core.

Jon J. Hangeland, Todd J. Friends, Arthur M. Doweyko, Karin Mellstroem, Johnny Sandberg, Marlena Grynfarb, Denis E. Ryono

Journal:

Année:

2005

Fichier:

PDF, 29 KB

2005

4

Steroid nuclear hormone receptors: The allosteric conversation

Arthur M. Doweyko

Journal:

Drug Development Research

Année:

2007

Langue:

english

Fichier:

PDF, 555 KB

english, 2007

5

Discovery of novel dihydro-9,10-ethano-anthracene carboxamides as glucocorticoid receptor modulators

Bingwei V. Yang, Wayne Vaccaro, Arthur M. Doweyko, Lidia M. Doweyko, Tram Huynh, David Tortolani, Steven G. Nadler, Lorraine McKay, John Somerville, Deborah A. Holloway, Sium Habte, David S. Weinstein

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2009

Langue:

english

Fichier:

PDF, 840 KB

english, 2009

6

Estimation of hERG inhibition of drug candidates using multivariate property and pharmacophore SAR

Stephen R. Johnson, Hongwen Yue, Mary Lee Conder, Hong Shi, Arthur M. Doweyko, John Lloyd, Paul Levesque

Journal:

Bioorganic & Medicinal Chemistry

Année:

2007

Langue:

english

Fichier:

PDF, 380 KB

english, 2007

7

Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56Lck

John Wityak, Jagabandhu Das, Robert V. Moquin, Zhongqi Shen, James Lin, Ping Chen, Arthur M. Doweyko, Sidney Pitt, Suhong Pang, Ding Ren Shen, Qiong Fang, Henry F. de Fex, Gary L. Schieven, Steven B.

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2003

Langue:

english

Fichier:

PDF, 224 KB

english, 2003

8

N-[1-Aryl-2-(1-imidazolo)ethyl]-guanidine derivatives as potent inhibitors of the bovine mitochondrial F1F0 ATP hydrolase

Karnail S. Atwal, Saleem Ahmad, Charles Z. Ding, Philip D. Stein, John Lloyd, Lawrence G. Hamann, David W. Green, Francis N. Ferrara, Paulina Wang, W.Lynn Rogers, Lidia M. Doweyko, Arthur V. Miller, S

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2004

Langue:

english

Fichier:

PDF, 175 KB

english, 2004

9

Thyroid receptor ligands. Part 2: Thyromimetics with improved selectivity for the thyroid hormone receptor beta

Jon J. Hangeland, Arthur M. Doweyko, Tamara Dejneka, Todd J. Friends, Pratik Devasthale, Karin Mellström, Johnny Sandberg, Marlena Grynfarb, John S. Sack, Howard Einspahr, Mathias Färnegårdh, Bolette

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2004

Langue:

english

Fichier:

PDF, 580 KB

english, 2004

10

A new class of high affinity thyromimetics containing a phenyl-naphthylene core

Jon J. Hangeland, Todd J. Friends, Arthur M. Doweyko, Karin Mellström, Johnny Sandberg, Marlena Grynfarb, Denis E. Ryono

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2005

Langue:

english

Fichier:

PDF, 189 KB

english, 2005

11

Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors

Jagabandhu Das, Joseph A. Furch, Chunjian Liu, Robert V. Moquin, James Lin, Steven H. Spergel, Kim W. McIntyre, David J. Shuster, Kathleen D. O’Day, Becky Penhallow, Chen-Yi Hung, Arthur M. Doweyko, A

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2006

Langue:

english

Fichier:

PDF, 152 KB

english, 2006

12

Corrigendum to “Discovery and SAR of 2-amino-5-[(thiomethyl)aryl]thiazoles as potent and selective Itk inhibitors” [Bioorg. Med. Chem. Lett. 16 (2006) 2411–2415]

Jagabandhu Das, Chunjian Liu, Robert V. Moquin, James Lin, Joseph A. Furch, Steven H. Spergel, Arthur M. Doweyko, Kim W. McIntyre, David J. Shuster, Kathleen D. O’Day, Becky Penhallow, Chen-Yi Hung, S

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2006

Fichier:

PDF, 50 KB

2006

13

Synthesis and SAR of p38α MAP kinase inhibitors based on heterobicyclic scaffolds

T.G. Murali Dhar, Stephen T. Wrobleski, Shuqun Lin, Joseph A. Furch, David S. Nirschl, Yi Fan, Gordon Todderud, Sidney Pitt, Arthur M. Doweyko, John S. Sack, Arvind Mathur, Murray McKinnon, Joel C. Ba

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2007

Langue:

english

Fichier:

PDF, 307 KB

english, 2007

14

Benzothiazole based inhibitors of p38α MAP kinase

Chunjian Liu, James Lin, Sidney Pitt, Rosemary F. Zhang, John S. Sack, Susan E. Kiefer, Kevin Kish, Arthur M. Doweyko, Hongjian Zhang, Punit H. Marathe, James Trzaskos, Murray Mckinnon, John H. Dodd,

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2008

Langue:

english

Fichier:

PDF, 202 KB

english, 2008

15

Synthesis and SAR of new pyrrolo[2,1-f][1,2,4]triazines as potent p38α MAP kinase inhibitors

Stephen T. Wrobleski, Shuqun Lin, John Hynes Jr., Hong Wu, Sidney Pitt, Ding Ren Shen, Rosemary Zhang, Kathleen M. Gillooly, David J. Shuster, Kim W. McIntyre, Arthur M. Doweyko, Kevin F. Kish, Jeffre

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2008

Langue:

english

Fichier:

PDF, 251 KB

english, 2008

16

Pyrazolo-pyrimidines: A novel heterocyclic scaffold for potent and selective p38α inhibitors

Jagabandhu Das, Robert V. Moquin, Sidney Pitt, Rosemary Zhang, Ding Ren Shen, Kim W. McIntyre, Kathleen Gillooly, Arthur M. Doweyko, John S. Sack, Hongjian Zhang, Susan E. Kiefer, Kevin Kish, Murray M

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2008

Langue:

english

Fichier:

PDF, 274 KB

english, 2008

17

Utilization of a nitrogen–sulfur nonbonding interaction in the design of new 2-aminothiazol-5-yl-pyrimidines as p38α MAP kinase inhibitors

Shuqun Lin, Stephen T. Wrobleski, John Hynes Jr., Sidney Pitt, Rosemary Zhang, Yi Fan, Arthur M. Doweyko, Kevin F. Kish, John S. Sack, Mary F. Malley, Susan E. Kiefer, John A. Newitt, Murray McKinnon,

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2010

Langue:

english

Fichier:

PDF, 770 KB

english, 2010

18

5-Amino-pyrazoles as potent and selective p38α inhibitors

Jagabandhu Das, Robert V. Moquin, Alaric J. Dyckman, Tianle Li, Sidney Pitt, Rosemary Zhang, Ding Ren Shen, Kim W. McIntyre, Kathleen Gillooly, Arthur M. Doweyko, John A. Newitt, John S. Sack, Hongjia

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2010

Langue:

english

Fichier:

PDF, 1.29 MB

english, 2010

19

The alkylation and halogenation of sulfones : Catalyzed by hydroxide ion in aprotic solvents

Richard R. Regis, Arthur M. Doweyko

Journal:

Tetrahedron Letters

Année:

1982

Langue:

english

Fichier:

PDF, 211 KB

english, 1982

20

Molecular design, synthesis, and structure–Activity relationships leading to the potent and selective p56lck inhibitor BMS-243117

Jagabandhu Das, James Lin, Robert V. Moquin, Zhongqi Shen, Steven H. Spergel, John Wityak, Arthur M. Doweyko, Henry F. DeFex, Qiong Fang, Suhong Pang, Sidney Pitt, Ding Ren Shen, Gary L. Schieven, Joe

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2003

Langue:

english

Fichier:

PDF, 228 KB

english, 2003

21

Discovery of 2-amino-heteroaryl-benzothiazole-6-anilides as potent p56lck inhibitors

Jagabandhu Das, Robert V. Moquin, James Lin, Chunjian Liu, Arthur M. Doweyko, Henry F. DeFex, Qiong Fang, Suhong Pang, Sidney Pitt, Ding Ren Shen, Gary L. Schieven, Joel C. Barrish, John Wityak

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2003

Langue:

english

Fichier:

PDF, 204 KB

english, 2003

22

3D-QSAR illusions

Arthur M. Doweyko

Journal:

Journal of Computer-Aided Molecular Design

Année:

2004

Langue:

english

Fichier:

PDF, 300 KB

english, 2004

23

QSAR: dead or alive?

Arthur M. Doweyko

Journal:

Journal of Computer-Aided Molecular Design

Année:

2008

Langue:

english

Fichier:

PDF, 474 KB

english, 2008

24

Corrigendum to “A new class of high affinity thyromimetics containing a phenyl-naphthylene core” [Bioorg. Med. Chem. Lett. 15 (2005) 4579–4584]

Jon J. Hangeland, Todd J. Friends, Arthur M. Doweyko, Karin Mellström, Johnny Sandberg, Marlena Grynfarb, Denis E. Ryono

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2006

Langue:

english

Fichier:

PDF, 58 KB

english, 2006

25

Comparison of 3D quantitative structure-activity relationship methods: Analysis of the in vitro antimalarial activity of 154 artemisinin analogues by hypothetical active-site lattice and comparative molecular field analysis

John R. Woolfrey, Mitchell A. Avery, Arthur M. Doweyko

Journal:

Journal of Computer-Aided Molecular Design

Année:

1998

Langue:

english

Fichier:

PDF, 178 KB

english, 1998

26

3D-QSAR using `Multiconformer' alignment: The use of HASL in the analysis of 5-HT1A thienopyrimidinone ligands

Salvatore Guccione, Arthur M. Doweyko, Hongming Chen, GloriaUccello Barretta, Federica Balzano

Journal:

Journal of Computer-Aided Molecular Design

Année:

2000

Langue:

english

Fichier:

PDF, 196 KB

english, 2000

27

Dimethyl-diphenyl-propanamide Derivatives As Nonsteroidal Dissociated Glucocorticoid Receptor Agonists

Yang, Bingwei V., Weinstein, David S., Doweyko, Lidia M., Gong, Hua, Vaccaro, Wayne, Huynh, Tram, Xiao, Hai-yun, Doweyko, Arthur M., Mckay, Lorraine, Holloway, Deborah A.

Journal:

Journal of Medicinal Chemistry

Année:

2010

Langue:

english

Fichier:

PDF, 2.24 MB

english, 2010

28

2-Aminothiazole as a Novel Kinase Inhibitor Template. Structure−Activity Relationship Studies toward the Discovery of N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (Dasatinib, BMS-354825) as a Potent pan-Src Kinase Inhibitor

Das, Jagabandhu, Chen, Ping, Norris, Derek, Padmanabha, Ramesh, Lin, James, Moquin, Robert V., Shen, Zhongqi, Cook, Lynda S., Doweyko, Arthur M., Pitt, Sidney

Journal:

Journal of Medicinal Chemistry

Année:

2006

Langue:

english

Fichier:

PDF, 396 KB

english, 2006

29

Pharmacophores from Binding Data

Doweyko, Arthur M.

Journal:

Journal of Medicinal Chemistry

Année:

1994

Langue:

english

Fichier:

PDF, 2.52 MB

english, 1994

30

Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38α MAP kinase inhibitors

Alaric J. Dyckman, Tianle Li, Sidney Pitt, Rosemary Zhang, Ding Ren Shen, Kim W. McIntyre, Kathleen M. Gillooly, David J. Shuster, Arthur M. Doweyko, John S. Sack, Kevin Kish, Susan E. Kiefer, John A.

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2011

Langue:

english

Fichier:

PDF, 948 KB

english, 2011

31

Antiulcer Agents. 6. Analysis of the in Vitro Biochemical and in Vivo Gastric Antisecretory Activity of Substituted Imidazo[1,2- a ]pyridines and Related Analogues Using Comparative Molecular Field Analysis and Hypothetical Active Site Lattice Methodologies

Kaminski, James J., Doweyko, Arthur M.

Journal:

Journal of Medicinal Chemistry

Année:

1997

Langue:

english

Fichier:

PDF, 324 KB

english, 1997

32

Discovery of N -(2-Chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a Dual Src/Abl Kinase Inhibitor with Potent Antitumor Activity in Preclinical Assays

Lombardo, Louis J., Lee, Francis Y., Chen, Ping, Norris, Derek, Barrish, Joel C., Behnia, Kamelia, Castaneda, Stephen, Cornelius, Lyndon A. M., Das, Jagabandhu, Doweyko, Arthur M., Fairchild, Craig, H

Journal:

Journal of Medicinal Chemistry

Année:

2004

Langue:

english

Fichier:

PDF, 307 KB

english, 2004

33

An application of 3D-QSAR to the analysis of the sequence specificity of DNA alkylation by uracil mustard

Doweyko, Arthur M., Mattes, William B.

Journal:

Année:

1992

Langue:

english

Fichier:

PDF, 1.47 MB

english, 1992

34

Azaxanthene Based Selective Glucocorticoid Receptor Modulators: Design, Synthesis, and Pharmacological Evaluation of ( S )-4-(5-(1-((1,3,4-Thiadiazol-2-yl)amino)-2-methyl-1-oxopropan-2-yl)-5 H -chromeno[2,3- b ]pyridin-2-yl)-2-fluoro- N , N -dimethylbenzamide (BMS-776532) and Its Methylene Homologue (BMS-791826)

Weinstein, David S., Gong, Hua, Doweyko, Arthur M., Cunningham, Mark, Habte, Sium, Wang, Jin Hong, Holloway, Deborah A., Burke, Christine, Gao, Ling, Guarino, Victor, Carman, Julie, Somerville, John E

Journal:

Journal of Medicinal Chemistry

Année:

2011

Langue:

english

Fichier:

PDF, 2.96 MB

english, 2011

35

Glyoxalase I enzyme studies. 3. Synthesis and evaluation of .alpha.-hydroxythiol esters as antitumor agents and glyoxalase I inhibitors

Hall, Stan S., Doweyko, Lidia M., Doweyko, Arthur M., Zilenovski, Judith S. Ryan

Journal:

Journal of Medicinal Chemistry

Année:

1977

Langue:

english

Fichier:

PDF, 559 KB

english, 1977

36

Synthesis and structure–activity relationships of novel indazolyl glucocorticoid receptor partial agonists

Gilmore, John L., Sheppeck, James E., Wang, Jim, Dhar, T.G. Murali, Cavallaro, Cullen, Doweyko, Arthur M., Mckay, Lorraine, Cunningham, Mark D., Habte, Sium F., Nadler, Steven G., Dodd, John H., Somer

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2013

Langue:

english

Fichier:

PDF, 659 KB

english, 2013

37

Discovery of potent and selective nonsteroidal indazolyl amide glucocorticoid receptor agonists

Sheppeck, James E., Gilmore, John L., Xiao, Hai-Yun, Dhar, T.G. Murali, Nirschl, David, Doweyko, Arthur M., Sack, Jack S., Corbett, Martin J., Malley, Mary F., Gougoutas, Jack Z., Mckay, Lorraine, Cun

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2013

Langue:

english

Fichier:

PDF, 1019 KB

english, 2013

38

The identification of novel p38α isoform selective kinase inhibitors having an unprecedented p38α binding mode

Wrobleski, Stephen T., Lin, Shuqun, Murali Dhar, T.G., Dyckman, Alaric J., Li, Tianle, Pitt, Sidney, Zhang, Rosemary, Fan, Yi, Doweyko, Arthur M., Tokarski, John S., Kish, Kevin F., Kiefer, Susan E.,

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2013

Langue:

english

Fichier:

PDF, 2.06 MB

english, 2013

39

Discovery of acylurea isosteres of 2-acylaminothiadiazole in the azaxanthene series of glucocorticoid receptor agonists

Gong, Hua, Yang, Michael, Xiao, Zili, Doweyko, Arthur M., Cunningham, Mark, Wang, Jinhong, Habte, Sium, Holloway, Deborah, Burke, Christine, Shuster, David, Gao, Ling, Carman, Julie, Somerville, John

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2014

Langue:

english

Fichier:

PDF, 1.49 MB

english, 2014

40

Glyoxalase I enzyme studies. 4. General base catalyzed enediol proton transfer rearrangement of methyl- and phenylglyoxalglutathionylhemithiol acetal to S-lactoyl- and S-mandeloylglutathione followed by hydrolysis. A model for the glyoxalase enzyme system

Hall, Stan S., Doweyko, Arthur M., Jordan, Frank

Journal:

Journal of the American Chemical Society

Année:

1978

Langue:

english

Fichier:

PDF, 767 KB

english, 1978

41

A novel class of fungicides: (2-pyridylthio)methyl benzoate N-oxides

Stanton, David T., Davis, Robert A., Doweyko, Arthur M.

Journal:

Journal of Agricultural and Food Chemistry

Année:

1983

Langue:

english

Fichier:

PDF, 390 KB

english, 1983

42

Imidazoquinoxaline Src-Family Kinase p56 Lck Inhibitors: SAR, QSAR, and the Discovery of ( S )- N -(2-Chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5- a ]pyrido[3,2- e ]pyrazin-6-amine (BMS-279700) as a Potent and Orally Active Inhibitor with Excellent in Vivo Antiinflammatory Activity

Chen, Ping, Doweyko, Arthur M., Norris, Derek, Gu, Henry H., Spergel, Steven H., Das, Jagabundhu, Moquin, Robert V., Lin, James, Wityak, John, Iwanowicz, Edwin J., McIntyre, Kim W., Shuster, David J.,

Journal:

Journal of Medicinal Chemistry

Année:

2004

Langue:

english

Fichier:

PDF, 370 KB

english, 2004

43

A Novel Method to Simulate the Hydrophobic Effect and Its Application to the Ranking of Host/Guest Complexes

Doweyko, Arthur M., Johnson, Stephen R.

Journal:

Journal of Chemical Information and Modeling

Année:

2006

Langue:

english

Fichier:

PDF, 1.26 MB

english, 2006

44

Quantitative structure-activity relationships for 2-[(phenylmethyl)sulfonyl]pyridine 1-oxide herbicides

Doweyko, Arthur M., Bell, Allyn R., Minatelli, John A., Relyea, Douglas I.

Journal:

Journal of Medicinal Chemistry

Année:

1983

Langue:

english

Fichier:

PDF, 561 KB

english, 1983

45

The hypothetical active site lattice. An approach to modelling active sites from data on inhibitor molecules

Doweyko, Arthur M.

Journal:

Journal of Medicinal Chemistry

Année:

1988

Langue:

english

Fichier:

PDF, 2.11 MB

english, 1988

46

Glyoxalase I enzyme studies. 2. Nuclear magnetic resonance evidence for an enediol-proton transfer mechanism

Hall, Stan S., Doweyko, Arthur M., Jordan, Frank

Journal:

Journal of the American Chemical Society

Année:

1976

Langue:

english

Fichier:

PDF, 252 KB

english, 1976

47

THE SYNTHESIS AND BIOLOGICAL ACTIVITY OF S-ALKYL PHOSPHOHOMOCYSTEINE SULFOXIMIDES

Nowakowski, Mark, Tishler, Max, Doweyko, Arthur M.

Journal:

Phosphorus Sulfur and Silicon and the Related Elements

Année:

1989

Langue:

english

Fichier:

PDF, 377 KB

english, 1989