Volume 14; Issue 19

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Bioorganic & Medicinal Chemistry Letters
Volume 14; Issue 19

Bioorganic & Medicinal Chemistry Letters

Volume 14; Issue 19

1

P4 and P1′ optimization of bicycloproline P2 bearing tetrapeptidyl α-ketoamides as HCV protease inhibitors

Yvonne Yip, Frantz Victor, Jason Lamar, Robert Johnson, Q. May Wang, John I. Glass, Nathan Yumibe, Mark Wakulchik, John Munroe, Shu-Hui Chen

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 278 KB

english, 2004

2

Synthesis of ether analogues derived from HUN-7293 and evaluation as inhibitors of VCAM-1 expression

Erwin P. Schreiner, Michael Kern, Andrea Steck, Carolyn A. Foster

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 275 KB

english, 2004

3

Estrone formate: a novel type of irreversible inhibitor of human steroid sulfatase

Erwin P. Schreiner, Andreas Billich

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 272 KB

english, 2004

4

Synthesis of dimeric acridine derived antivirals

René Csuk, Alexander Barthel, Torsten Brezesinski, Christian Raschke

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 249 KB

english, 2004

5

Steroid and lipid conjugates of siRNAs to enhance cellular uptake and gene silencing in liver cells

Christina Lorenz, Philipp Hadwiger, Matthias John, Hans-Peter Vornlocher, Carlo Unverzagt

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 330 KB

english, 2004

6

Effective inhibition of HIV-1 replication in cultured cells by external guide sequences and ribonuclease P

Jacob S. Barnor, Yumihiko Endo, Yuichiro Habu, Naoko Miyano-Kurosaki, Michiko Kitano, Hirokazu Yamamoto, Hiroshi Takaku

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 352 KB

english, 2004

7

Synthesis of benzimidazole based analogues of sphingosine-1-phosphate: discovery of potent, subtype-selective S1P4 receptor agonists

Jeremy J. Clemens, Michael D. Davis, Kevin R. Lynch, Timothy L. Macdonald

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 350 KB

english, 2004

8

Discovery of orally active prostaglandin D2 receptor antagonists

Kazuhiko Torisu, Kaoru Kobayashi, Maki Iwahashi, Yoshihiko Nakai, Takahiro Onoda, Toshihiko Nagase, Isamu Sugimoto, Yutaka Okada, Ryoji Matsumoto, Fumio Nanbu, Shuichi Ohuchida, Hisao Nakai, Masaaki T

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 276 KB

english, 2004

9

Design and synthesis of 3′-ureidoadenosine-5′-uronamides: effects of the 3′-ureido group on binding to the A3 adenosine receptor

Lak Shin Jeong, Myong Jung Kim, Hea Ok Kim, Zhan-Guo Gao, Soo-Kyung Kim, Kenneth A. Jacobson, Moon Woo Chun

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 298 KB

english, 2004

10

Pyridazine derivatives and related compounds. Part 13: Synthesis and antimicrobial activity of some pyridazino[3′,4′:3,4]pyrazolo[5,1-c]-1,2,4-triazines

Ali Deeb, Fatma El-Mariah, Mona Hosny

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 274 KB

english, 2004

11

Synthesis of acyloxymethyl ester prodrugs of the transferable protein farnesyl transferase substrate farnesyl methylenediphosphonate

Jerry M. Troutman, Kareem A.H. Chehade, Katarzyna Kiegiel, Douglas A. Andres, H. Peter Spielmann

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 273 KB

english, 2004

12

Asymmetric synthesis of the stereoisomers of 11,12,15(S)-trihydroxyeicosa-5(Z),8(Z),13(E)-trienoic acid, a potent endothelium-derived vasodilator

J.R. Falck, Deb Barma, Suchismita Mohapatra, A. Bandyopadhyay, Komandla Malla Reddy, Jianjun Qi, William Campbell

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 271 KB

english, 2004

13

Synthesis and structure–activity relationships of uracil derived human GnRH receptor antagonists: (R)-3-[2-(2-amino)phenethyl]-1-(2,6-difluorobenzyl)-6-methyluracils containing a substituted thiophene or thiazole at C-5

Martin W. Rowbottom, Fabio C. Tucci, Patrick J. Connors Jr, Timothy D. Gross, Yun-Fei Zhu, Zhiqiang Guo, Manisha Moorjani, Oscar Acevedo, Lee Carter, Susan K. Sullivan, Qiu Xie, Andrew Fisher, R. Scot

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 306 KB

english, 2004

14

The development of new bicyclic pyrazole-based cytokine synthesis inhibitors

Jennifer A. Townes, Adam Golebiowski, Michael P. Clark, Matthew J. Laufersweiler, Todd A. Brugel, Mark Sabat, Roger G. Bookland, Steve K. Laughlin, John C. VanRens, Biswanath De, Lily C. Hsieh, Susan

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 313 KB

english, 2004

15

Synthesis and biological evaluation of novel cytotoxic phospholipids for prostate cancer

Veeresa Gududuru, Eunju Hurh, Gangadhar G. Durgam, Seoung Soo Hong, Vineet M. Sardar, Huiping Xu, James T. Dalton, Duane D. Miller

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 274 KB

english, 2004

16

A new class of acyclic 2-alkyl-1,2-diaryl (E)-olefins as selective cyclooxygenase-2 (COX-2) inhibitors

Md. Jashim Uddin, P.N. Praveen Rao, Md. Abdur Rahim, Robert McDonald, Edward E. Knaus

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 328 KB

english, 2004

17

Potent and selective P2–P3 ketoamide inhibitors of cathepsin K with good pharmacokinetic properties via favorable P1′, P1, and/or P3 substitutions

David G. Barrett, John G. Catalano, David N. Deaton, Anne M. Hassell, Stacey T. Long, Aaron B. Miller, Larry R. Miller, Lisa M. Shewchuk, Kevin J. Wells-Knecht, Derril H. Willard Jr., Lois L. Wright

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 341 KB

english, 2004

18

Synthesis and GABA receptor potency of 3-thiomethyl-4-(hetero)aryl-5-amino-1-phenylpyrazoles

Sanath K. Meegalla, Dario Doller, DeYou Sha, Rich Soll, Nancy Wisnewski, Gary M. Silver, Dale Dhanoa

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 276 KB

english, 2004

19

Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 2

Anil Vasudevan, Dariusz Wodka, Mary K. Verzal, Andrew J. Souers, Ju Gao, Sevan Brodjian, Dennis Fry, Brian Dayton, Kennan C. Marsh, Lisa E. Hernandez, Christopher A. Ogiela, Christine A. Collins, Phil

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 266 KB

english, 2004

20

Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 3

Andrew J. Souers, Dariusz Wodka, Ju Gao, Jared C. Lewis, Anil Vasudevan, Sevan Brodjian, Brian Dayton, Christopher A. Ogiela, Dennis Fry, Lisa E. Hernandez, Kennan C. Marsh, Christine A. Collins, Phil

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 268 KB

english, 2004

21

Pyrrolo[2,1-c][1,4]benzodiazepine–anthraquinone conjugates. Synthesis, DNA binding and cytotoxicity

Ahmed Kamal, R. Ramu, G.B. Ramesh Khanna, Ajit Kumar Saxena, M. Shanmugavel, Renu Moti Pandita

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 261 KB

english, 2004

22

Study on noncovalent complexes of cytotoxic protoberberine alkaloids with double-stranded DNA by using electrospray ionization mass spectrometry

Wen-Hua Chen, Chi-Leung Chan, Zongwei Cai, Guo-An Luo, Zhi-Hong Jiang

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 556 KB

english, 2004

23

Modeling the binding affinities of β-secretase inhibitors: application to subsite specificity

Ramkumar Rajamani, Charles H. Reynolds

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 283 KB

english, 2004

24

Design and synthesis of conformationally constrained 3-(N-alkylamino)propylphosphonic acids as potent agonists of sphingosine-1-phosphate (S1P) receptors

Lin Yan, Jeffrey J. Hale, Christopher L. Lynch, Richard Budhu, Amy Gentry, Sander G. Mills, Richard Hajdu, Carol Ann Keohane, Mark J. Rosenbach, James A. Milligan, Gan-Ju Shei, Gary Chrebet, James Ber

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 306 KB

english, 2004

25

Inhibition of the strand transfer step of HIV-1 integrase by non-natural dinucleotides

Guochen Chi, Nouri Neamati, Vasu Nair

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 261 KB

english, 2004

26

Novel pyrazinone inhibitors of mast cell tryptase: synthesis and SAR evaluation

Corey Hopkins, Kent Neuenschwander, Anthony Scotese, Sharon Jackson, Thaddeus Nieduzak, Henry Pauls, Guyan Liang, Keith Sides, Dona Cramer, Jennifer Cairns, Sebastien Maignan, Magali Mathieu

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 358 KB

english, 2004

27

Computational comparison of microtubule-stabilising agents laulimalide and peloruside with taxol and colchicine

Oriol Pineda, Jaume Farràs, Laura Maccari, Fabrizio Manetti, Maurizio Botta, Jaume Vilarrasa

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 484 KB

english, 2004

28

Editorial board

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

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PDF, 390 KB

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29

Graphical contents list

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

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PDF, 604 KB

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30

Contributors to this issue

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

File:

PDF, 189 KB

2004

31

Instructions to contributors

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 71 KB

english, 2004

32

Synthesis and vasorelaxant properties of hybrid molecules out of NO-donors and the β-receptor blocking drug propranolol

Michael Decker, Andreas König, Erika Glusa, Jochen Lehmann

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 270 KB

english, 2004

33

Synthesis of enantiomerically pure d-FDOC, an anti-HIV agent

Shuli Mao, Martin Bouygues, Christopher Welch, Mirlinda Biba, Jen Chilenski, Raymond F. Schinazi, Dennis C. Liotta

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 296 KB

english, 2004

34

Synthesis, structural properties and insulin-enhancing potential of bis(quercetinato)oxovanadium(IV) conjugate

Ruchi Shukla, Vivek Barve, Subhash Padhye, Ramesh Bhonde

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 291 KB

english, 2004

35

Synthesis and evaluation of novel oxazoline MMP inhibitors

Gregory R. Cook, Ethirajan Manivannan, Thane Underdahl, Viera Lukacova, Yufen Zhang, Stefan Balaz

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 324 KB

english, 2004

36

Synthesis and evaluation of 4-(1-aminoalkyl)-N-(4-pyridyl)cyclohexanecarboxamides as Rho kinase inhibitors and neurite outgrowth promoters

Karine Gingras, Hovsep Avedissian, Eryk Thouin, Véronique Boulanger, Charles Essagian, Lisa McKerracher, William D. Lubell

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 362 KB

english, 2004

37

The identification and optimization of 2,4-diketobutyric acids as flap endonuclease 1 inhibitors

L. Nathan Tumey, Bayard Huck, Elizabeth Gleason, Jianmin Wang, Daniel Silver, Kurt Brunden, Sherry Boozer, Stephen Rundlett, Bruce Sherf, Steven Murphy, Andrew Bailey, Tom Dent, Christina Leventhal, J

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 266 KB

english, 2004

38

7-Substituted 2-phenyl-benzofurans as ERβ selective ligands

Michael D. Collini, David H. Kaufman, Eric S. Manas, Heather A. Harris, Ruth A. Henderson, Zhang B. Xu, Rayomand J. Unwalla, Chris P. Miller

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 297 KB

english, 2004

39

Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 1

Andrew J. Souers, Dariusz Wodka, Ju Gao, Jared C. Lewis, Anil Vasudevan, Robert Gentles, Sevan Brodjian, Brian Dayton, Christopher A. Ogiela, Dennis Fry, Lisa E. Hernandez, Kennan C. Marsh, Christine

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 281 KB

english, 2004

40

Unnatural base pairs between 2- and 6-substituted purines and 2-oxo(1H)pyridine for expansion of the genetic alphabet

Ichiro Hirao, Tsuyoshi Fujiwara, Michiko Kimoto, Shigeyuki Yokoyama

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 269 KB

english, 2004

41

Identification of 4-piperazin-1-yl-quinazoline template based aryl and benzyl thioureas as potent, selective, and orally bioavailable inhibitors of platelet-derived growth factor (PDGF) receptor

Julie A. Heath, Mukund M. Mehrotra, Shannon Chi, Jin-Chen Yu, Athiwat Hutchaleelaha, Stanley J. Hollenbach, Neill A. Giese, Robert M. Scarborough, Anjali Pandey

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 317 KB

english, 2004

42

New DNA binding ligands as a model of chromomycin A3

Shuhei Imoto, Yoshinari Haruta, Kyouichi Watanabe, Shigeki Sasaki

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 377 KB

english, 2004

43

N-(1-Benzylpyrrolidin-3-yl)arylbenzamides as potent and selective human dopamine D4 antagonists

Ian Egle, Nancy Barriault, Michel Bordeleau, Jillian Drage, Laurence Dube, Jack Peragine, Lucy Mazzocco, Jalaj Arora, Keith Jarvie, Ashok Tehim

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 259 KB

english, 2004

44

End-capping of the modified melanocortin tetrapeptide (p-Cl)Phe-D-Phe-Arg-Trp-NH2 as a route to hMC4R agonists

L.N. Koikov, F.H. Ebetino, J.C. Hayes, D. Cross-Doersen, J.J. Knittel

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 267 KB

english, 2004

45

Studies on adenosine A2a receptor antagonists: comparison of three core heterocycles

Chi B. Vu, Deborah Pan, Bo Peng, Li Sha, Gnanasambandam Kumaravel, Xiaowei Jin, Deepali Phadke, Thomas Engber, Carol Huang, Jennifer Reilly, Stacy Tam, Russell C. Petter

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 273 KB

english, 2004

46

Triamino derivatives of triazolotriazine and triazolopyrimidine as adenosine A2a receptor antagonists

Chi B. Vu, Pamela Shields, Bo Peng, Gnanasambandam Kumaravel, Xiaowei Jin, Deepali Phadke, Joy Wang, Thomas Engber, Eman Ayyub, Russell C. Petter

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 266 KB

english, 2004