Volume 15; Issue 21

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Bioorganic & Medicinal Chemistry Letters
Volume 15; Issue 21

Bioorganic & Medicinal Chemistry Letters

Volume 15; Issue 21

1

Conformationally restricted anti-plasmodial chalcones

Mogens Larsen, Hasse Kromann, Arsalan Kharazmi, Simon Feldbæk Nielsen

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 134 KB

english, 2005

2

Camptothecin binds to a synthetic peptide identified by a T7 phage display screen

Yoichi Takakusagi, Susumu Kobayashi, Fumio Sugawara

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 151 KB

english, 2005

3

Synthesis of a biotinylated camptothecin derivative and determination of the binding sequence by T7 phage display technology

Yoichi Takakusagi, Keisuke Ohta, Kouji Kuramochi, Kengo Morohashi, Susumu Kobayashi, Kengo Sakaguchi, Fumio Sugawara

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 156 KB

english, 2005

4

Synthesis of potent and selective serotonin 5-HT1B receptor ligands

Yiyun Huang, Sung-A Bae, Bryan L. Roth, Marc Laruelle

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 116 KB

english, 2005

5

Trifluoromethyl group as a pharmacophore: Effect of replacing a CF3 group on binding and agonist activity of a glucocorticoid receptor ligand

Raj Betageri, Yan Zhang, Renee M. Zindell, Daniel Kuzmich, Thomas M. Kirrane, Jörg Bentzien, Mario Cardozo, Alison J. Capolino, Tazmeen N. Fadra, Richard M. Nelson, Zofia Paw, Daw-Tsun Shih, Cheng-Kon

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 418 KB

english, 2005

6

New dual inhibitors of EGFR and HER2 protein tyrosine kinases

Brian E. Fink, Gregory D. Vite, Harold Mastalerz, John F. Kadow, Soong-Hoon Kim, Kenneth J. Leavitt, Karen Du, Donald Crews, Toomas Mitt, Tai W. Wong, John T. Hunt, Dolatrai M. Vyas, John S. Tokarski

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 176 KB

english, 2005

7

Conformationally constrained N1-arylsulfonyltryptamine derivatives as 5-HT6 receptor antagonists

Derek C. Cole, William J. Lennox, Joseph R. Stock, John W. Ellingboe, Hossein Mazandarani, Deborah L. Smith, Guoming Zhang, Gregory J. Tawa, Lee E. Schechter

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 164 KB

english, 2005

8

Potential antitumor agents: Flavones and their derivatives from Linaria reflexa Desf.

Rosa Tundis, Brigitte Deguin, Monica R. Loizzo, Marco Bonesi, Giancarlo A. Statti, François Tillequin, Francesco Menichini

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 106 KB

english, 2005

9

Investigation of factor Xa inhibitors containing non-amidine S1 elements

Jeffry B. Franciskovich, John J. Masters, Jennifer M. Tinsley, Trelia J. Craft, Larry L. Froelich, Donetta S. Gifford-Moore, Valentine J. Klimkowski, Jeffrey K. Smallwood, Gerald F. Smith, Tommy Smith

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 138 KB

english, 2005

10

Synthesis and evaluation of 18F-labeled dopamine D3 receptor ligands as potential PET imaging agents

Carsten Hocke, Olaf Prante, Stefan Löber, Harald Hübner, Peter Gmeiner, Torsten Kuwert

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 191 KB

english, 2005

11

Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective σ1 ligands. Part 2

Amaury Cazenave Gassiot, Julie Charton, Sophie Girault-Mizzi, Pauline Gilleron, Marie-Ange Debreu-Fontaine, Christian Sergheraert, Patricia Melnyk

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 151 KB

english, 2005

12

Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective σ1 ligands. Part 1

Julie Charton, Amaury Cazenave Gassiot, Sophie Girault-Mizzi, Marie-Ange Debreu-Fontaine, Patricia Melnyk, Christian Sergheraert

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 140 KB

english, 2005

13

Synthesis and anthelmintic properties of arylquinolines with activity against drug-resistant nematodes

Sharon Rossiter, Jean-Marie Péron, Philip J. Whitfield, Keith Jones

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 102 KB

english, 2005

14

Activity and QSAR study of baogongteng A and its derivatives as muscarinic agonists

Yin-Yao Niu, Li-Min Yang, Hui-Zhong Liu, Yong-Yao Cui, Liang Zhu, Ju-Mei Feng, Jian-Hua Yao, Hong-Zhuan Chen, Bo-Tao Fan, Ze-Nai Chen, Yang Lu

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 180 KB

english, 2005

15

Novel indole α-methylene-γ-lactones as potent inhibitors for AKT-mTOR signaling pathway kinases

Huasheng Ding, Chao Zhang, Xihan Wu, Chunhao Yang, Xiongwen Zhang, Jian Ding, Yuyuan Xie

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 151 KB

english, 2005

16

Novel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity

Jos H.M. Lange, Herman H. van Stuivenberg, Willem Veerman, Henri C. Wals, Bob Stork, Hein K.A.C. Coolen, Andrew C. McCreary, Tiny J.P. Adolfs, Chris G. Kruse

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 211 KB

english, 2005

17

Synthesis and biological evaluation of 1-amino-1,1-bisphosphonates derived from fatty acids against Trypanosoma cruzi targeting farnesyl pyrophosphate synthase

Sergio H. Szajnman, Esteban L. Ravaschino, Roberto Docampo, Juan B. Rodriguez

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 144 KB

english, 2005

18

Inhibition of Src kinase activity by 7-[(2,4-dichloro-5-methoxyphenyl)amino]-2-heteroaryl-thieno[3,2-b]pyridine-6-carbonitriles

Diane H. Boschelli, Biqi Wu, Ana Carolina Barrios Sosa, Joan J. Chen, Jennifer M. Golas, Frank Boschelli

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 113 KB

english, 2005

19

Benzyl ether structure–activity relationships in a series of ketopiperazine-based renin inhibitors

Noel A. Powell, Emma H. Clay, Daniel D. Holsworth, John W. Bryant, Michael J. Ryan, Mehran Jalaie, Jeremy J. Edmunds

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 169 KB

english, 2005

20

High affinity ligands for the α7 nicotinic receptor that show no cross-reactivity with the 5-HT3 receptor

S. Richard Baker, John Boot, Michael Brunavs, David Dobson, Rachel Green, Lorna Hayhurst, Martine Keenan, Louise Wallace

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 115 KB

english, 2005

21

Exploring the connection unit in the HDAC inhibitor pharmacophore model: Novel uracil-based hydroxamates

Antonello Mai, Silvio Massa, Dante Rotili, Riccardo Pezzi, Patrizia Bottoni, Roberto Scatena, Joachim Meraner, Gerald Brosch

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 334 KB

english, 2005

22

Neamine dimers targeting the HIV-1 TAR RNA

Emmanuel Riguet, Jérôme Désiré, Oliver Boden, Verena Ludwig, Michael Göbel, Christian Bailly, Jean-Luc Décout

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 131 KB

english, 2005

23

Bioisosteric phentolamine analogs as potent α-adrenergic antagonists

Seoung-Soo Hong, Supriya A. Bavadekar, Sang-Il Lee, Popat. N. Patil, S.G. Lalchandani, Dennis R. Feller, Duane D. Miller

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 119 KB

english, 2005

24

Density-functional theory studies on standard electrode potentials of half reaction for l-adrenaline and adrenalinequinone

Yuanzhi Song, JianFeng Zhou, Yang Song, Yongge Wei, Hong Wang

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 238 KB

english, 2005

25

Identification of a potent and selective 5-HT1B receptor antagonist

Paul A. Wyman, Howard R. Marshall, Sean T. Flynn, Ron J. King, Mervyn Thompson, Paul W. Smith, Michael S. Hadley, Gary W. Price, Claire M. Scott, Lee A. Dawson

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 132 KB

english, 2005

26

Announcing New European Regional Editor for Bioorganic & Medicinal Chemistry Letters

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 89 KB

english, 2005

27

Carbonic anhydrase inhibitors: Inhibition of the tumor-associated isozymes IX and XII with a library of aromatic and heteroaromatic sulfonamides

Özen Özensoy, Luca Puccetti, Giuseppe Fasolis, Oktay Arslan, Andrea Scozzafava, Claudiu T. Supuran

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 122 KB

english, 2005

28

Editorial Board

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 208 KB

english, 2005

29

Graphical contents list

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 514 KB

english, 2005

30

Contributors to this issue

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

File:

PDF, 190 KB

2005

31

Instructions to contributors

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 29 KB

english, 2005

32

Carbonic anhydrase inhibitors: Inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with benzo[b]thiophene 1,1-dioxide sulfonamides

Alessio Innocenti, Raquel Villar, Victor Martinez-Merino, María J. Gil, Andrea Scozzafava, Daniela Vullo, Claudiu T. Supuran

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 121 KB

english, 2005

33

Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT6 receptor antagonists

Mahmood Ahmed, Michael A. Briggs, Steven M. Bromidge, Tania Buck, Lorraine Campbell, Nigel J. Deeks, Ashley Garner, Laurie Gordon, Dieter W. Hamprecht, Vicky Holland, Christopher N. Johnson, Andrew D.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 260 KB

english, 2005

34

Synthesis and evaluation of 3-anilino-quinoxalinones as glycogen phosphorylase inhibitors

Joseph Dudash Jr., Yongzheng Zhang, John B. Moore, Richard Look, Yin Liang, Mary Pat Beavers, Bruce R. Conway, Philip J. Rybczynski, Keith T. Demarest

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 118 KB

english, 2005

35

New fluorinated pyrrolidine and azetidine amides as dipeptidyl peptidase IV inhibitors

Bernard Hulin, Shawn Cabral, Michael G. Lopaze, Maria A. Van Volkenburg, Kim M. Andrews, Janice C. Parker

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 113 KB

english, 2005

36

Synthesis and biological evaluation of 1,3-diphenylprop-2-yn-1-ones as dual inhibitors of cyclooxygenases and lipoxygenases

P.N. Praveen Rao, Qiao-Hong Chen, Edward E. Knaus

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 156 KB

english, 2005

37

A fluorogenic and chromogenic probe that detects the esterase activity of trace copper(II)

Radoslaw M. Kierat, Roland Krämer

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 141 KB

english, 2005

38

Synthesis and anticonvulsant activity of 7-alkoxyl-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolines

Zhi-Feng Xie, Kyu-Yun Chai, Hu-Ri Piao, Kyung-Chell Kwak, Zhe-Shan Quan

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 99 KB

english, 2005

39

Synthesis of [1,2,4]triazolo[1,5-a]pyrazines as adenosine A2A receptor antagonists

James E. Dowling, Jeffrey T. Vessels, Serajul Haque, He Xi Chang, Kurt van Vloten, Gnanasambandam Kumaravel, Thomas Engber, Xiaowei Jin, Deepali Phadke, Joy Wang, Eman Ayyub, Russell C. Petter

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 155 KB

english, 2005

40

SAR, species specificity, and cellular activity of cyclopentene dicarboxylic acid amides as DHODH inhibitors

Johann Leban, Martin Kralik, Jan Mies, Michael Gassen, Karin Tentschert, Roland Baumgartner

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 135 KB

english, 2005

41

Diamino-C,N-diarylpyridine positional isomers as inhibitors of lysophosphatidic acid acyltransferase-β

Feng Hong, David Hollenback, Jack W. Singer, Peter Klein

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 124 KB

english, 2005

42

The discovery of fluoropyridine-based inhibitors of the Factor VIIa/TF complex

Jeffrey T. Kohrt, Kevin J. Filipski, Wayne L. Cody, Cuiman Cai, Danette A. Dudley, Chad A. Van Huis, J. Adam Willardsen, Stephen T. Rapundalo, Kamlai Saiya-Cork, Robert J. Leadley, Lakshmi Narasimhan,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 199 KB

english, 2005

43

Arylphthalazines: Identification of a new phthalazine chemotype as inhibitors of VEGFR kinase

Evgueni L. Piatnitski, Matthew A.J. Duncton, Alexander S. Kiselyov, Reeti Katoch-Rouse, Dan Sherman, Daniel L. Milligan, Chris Balagtas, Wai C. Wong, Joel Kawakami, Jacqueline F. Doody

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 101 KB

english, 2005

44

Synthesis of 4-(5-[18F]fluoromethyl-3-phenylisoxazol-4-yl)benzenesulfonamide, a new [18F]fluorinated analogue of valdecoxib, as a potential radiotracer for imaging cyclooxygenase-2 with positron emission tomography

Tatsushi Toyokuni, J.S. Dileep Kumar, Joseph C. Walsh, Alan Shapiro, John J. Talley, Michael E. Phelps, Harvey R. Herschman, Jorge R. Barrio, Nagichettiar Satyamurthy

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 123 KB

english, 2005

45

Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 2. Structure–activity relationships of the 7- and 5-, 6-, 8-positions

William Kemnitzer, Shailaja Kasibhatla, Songchun Jiang, Hong Zhang, Jianghong Zhao, Shaojuan Jia, Lifen Xu, Candace Crogan-Grundy, Réal Denis, Nancy Barriault, Louis Vaillancourt, Sylvie Charron, Jenn

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 134 KB

english, 2005

46

Novel C2–C3′ N-peptide linked macrocyclic taxoids. Part 1: Synthesis and biological activities of docetaxel analogues with a peptide side chain at C3′

Anne-Laure Larroque, Joëlle Dubois, Sylviane Thoret, Geneviève Aubert, Daniel Guénard, Françoise Guéritte

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 298 KB

english, 2005

47

Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K

W. Cameron Black, Christopher I. Bayly, Dana E. Davis, Sylvie Desmarais, Jean-Pierre Falgueyret, Serge Léger, Chun Sing Li, Frédéric Massé, Daniel J. McKay, James T. Palmer, M. David Percival, Joël Ro

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 242 KB

english, 2005

48

Parallel synthesis and biological evaluation of 5,6,7,8-tetrahydrobenzothieno[2,3-d]pyrimidin-4(3H)-one cytotoxic agents selective for p21-deficient cells

Lee D. Jennings, Scott L. Kincaid, Yanong D. Wang, Girija Krishnamurthy, Carl F. Beyer, John P. McGinnis, Miriam Miranda, Carolyn M. Discafani, Sridhar K. Rabindran

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 147 KB

english, 2005

49

Total and semisynthesis and in vitro studies of both enantiomers of 20-fluorocamptothecin

Raghuram S. Tangirala, Rachel Dixon, Danzhou Yang, Attila Ambrus, Smitha Antony, Keli Agama, Yves Pommier, Dennis P. Curran

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 177 KB

english, 2005

50

The neuroprotective action of JNK3 inhibitors based on the 6,7-dihydro-5H-pyrrolo[1,2-a]imidazole scaffold

Piotr P. Graczyk, Afzal Khan, Gurpreet S. Bhatia, Vanessa Palmer, Darren Medland, Hirotoshi Numata, Hitoshi Oinuma, Jacqueline Catchick, Angela Dunne, Moira Ellis, Caroline Smales, Jonathan Whitfield,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 222 KB

english, 2005

51

Potential metabolites of a condensed 2,3-benzodiazepine derivative

Emese Csuzdi, Katalin Migléczi, István Hazai, Pál Berzsenyi, István Pallagi, Gyula Horváth, György Lengyel, Sándor Sólyom

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 114 KB

english, 2005

52

An efficient synthesis of argifin: A natural product chitinase inhibitor with chemotherapeutic potential

Mark J. Dixon, Ole A. Andersen, Daan M.F. van Aalten, Ian M. Eggleston

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 233 KB

english, 2005

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