Volume 15; Issue 5

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Bioorganic & Medicinal Chemistry Letters
Volume 15; Issue 5

Bioorganic & Medicinal Chemistry Letters

Volume 15; Issue 5

1

Isoindolinone-based inhibitors of the MDM2–p53 protein–protein interaction

Ian R. Hardcastle, Shafiq U. Ahmed, Helen Atkins, A. Hilary Calvert, Nicola J. Curtin, Gillian Farnie, Bernard T. Golding, Roger J. Griffin, Sabrina Guyenne, Claire Hutton, Per Källblad, Stuart J. Kem

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 221 KB

english, 2005

2

In vivo incorporation of an alkyne into proteins in Escherichia coli

Alexander Deiters, Peter G. Schultz

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 157 KB

english, 2005

3

Lysine derivatives as potent HIV protease inhibitors. Discovery, synthesis and structure–activity relationship studies

Abderrahim Bouzide, Gilles Sauvé, Jocelyn Yelle

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 138 KB

english, 2005

4

Synthesis and evaluation of diverse analogs of amygdalin as potential peptidomimetics of peptide T

Eyleen Araya, Alex Rodriguez, Jaime Rubio, Alessandro Spada, Jesus Joglar, Amadeu Llebaria, Carmen Lagunas, Andres G. Fernandez, Susanna Spisani, Juan J. Perez

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 127 KB

english, 2005

5

Synthesis and evaluation of azalanstat analogues as heme oxygenase inhibitors

Jason Z. Vlahakis, Robert T. Kinobe, Raymond J. Bowers, James F. Brien, Kanji Nakatsu, Walter A. Szarek

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 154 KB

english, 2005

6

Electronic structure calculations on the thiazole-containing antibiotic thiostrepton: molecular mechanics, semi-empirical and ab initio analyses

Pei C. Hang, John F. Honek

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 222 KB

english, 2005

7

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

Year:

2005

Language:

english

File:

PDF, 144 KB

english, 2005

8

Tryptamine and homotryptamine-based sulfonamides as potent and selective inhibitors of 15-lipoxygenase

David S. Weinstein, Wen Liu, Zhengxiang Gu, Charles Langevine, Khehyong Ngu, Leena Fadnis, Donald W. Combs, Doree Sitkoff, Saleem Ahmad, Shaobin Zhuang, Xing Chen, Feng-Lai Wang, Deborah A. Loughney,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 157 KB

english, 2005

9

Glucokinase-activating ureas

Arlindo L. Castelhano, Hanqing Dong, Matthew C.T. Fyfe, Lisa S. Gardner, Yukari Kamikozawa, Satomi Kurabayashi, Masao Nawano, Rikiya Ohashi, Martin J. Procter, Li Qiu, Chrystelle M. Rasamison, Karen L

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 128 KB

english, 2005

10

Structure–activity relationships of dimeric PPAR agonists

Per Sauerberg, John P. Mogensen, Lone Jeppesen, L. Anders Svensson, Jan Fleckner, Jan Nehlin, Erik M. Wulff, Ingrid Pettersson

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 181 KB

english, 2005

11

Discovery of an exceptionally potent and selective class of fatty acid amide hydrolase inhibitors enlisting proteome-wide selectivity screening: concurrent optimization of enzyme inhibitor potency and selectivity

Donmienne Leung, Wu Du, Christophe Hardouin, Heng Cheng, Inkyu Hwang, Benjamin F. Cravatt, Dale L. Boger

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 143 KB

english, 2005

12

Aglycon specificity profiling of α-glucosidases using synthetic probes

Wataru Hakamata, Makoto Muroi, Kazunari Kadokura, Toshiyuki Nishio, Tadatake Oku, Atsuo Kimura, Seiya Chiba, Akira Takatsuki

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 125 KB

english, 2005

13

3,4-Disubstituted azetidinones as selective inhibitors of the cysteine protease cathepsin K. Exploring P3 elements for potency and selectivity

Eduardo L. Setti, Dana Davis, James W. Janc, Douglas A. Jeffery, Harry Cheung, Walter Yu

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 141 KB

english, 2005

14

2-Substituted-4-aryl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,5]oxazocin-5-one as a structurally new NK1 antagonist

Shigeki Seto, Asao Tanioka, Makoto Ikeda, Shigeru Izawa

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 106 KB

english, 2005

15

New derivatives of 1α,25-dihydroxy-19-norvitamin D3 with two substituents at C-2: synthesis and biological activity

Masato Shimizu, Yukiko Iwasaki, Mika Shimazaki, Youhei Amano, Keiko Yamamoto, Wolfgang Reischl, Sachiko Yamada

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 131 KB

english, 2005

16

Design and synthesis of novel 9-substituted-7-aryl-3,4,5,6-tetrahydro-2H-pyrido[4,3-b]- and [2,3-b]-1,5-oxazocin-6-ones as NK1 antagonists

Shigeki Seto, Asao Tanioka, Makoto Ikeda, Shigeru Izawa

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 133 KB

english, 2005

17

Protein microarray using α-amino acids as metal tags on chips

Supachok Sinchaikul, Fu-Ming Pan, Ching-Wen Cheng, Chi-Huey Wong, Jim-Min Fang, Min-Jen Tseng, Shui-Tein Chen

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 191 KB

english, 2005

18

Discovery and investigation of a novel class of thiophene-derived antagonists of the human glucagon receptor

Joseph L. Duffy, Brian A. Kirk, Zenon Konteatis, Elizabeth L. Campbell, Rui Liang, Edward J. Brady, Mari Rios Candelore, Victor D.H. Ding, Guoqiang Jiang, Frank Liu, Sajjad A. Qureshi, Richard Saperst

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 137 KB

english, 2005

19

4-(2-Aminoethoxy)-N-(phenylsulfonyl)indoles as novel 5-HT6 receptor ligands

Ping Zhou, Yinfa Yan, Ronald Bernotas, Boyd L. Harrison, Donna Huryn, Albert J. Robichaud, Guo Ming Zhang, Deborah L. Smith, Lee E. Schechter

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 108 KB

english, 2005

20

Chemistry and biology of mercaptoacetamides as novel histone deacetylase inhibitors

Bin Chen, Pavel A. Petukhov, Mira Jung, Alfredo Velena, Elena Eliseeva, Anatoly Dritschilo, Alan P. Kozikowski

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 132 KB

english, 2005

21

Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: peptidomimetic replacement of the P2 α-amino acid by a α-hydroxy acid

Yan Wang, Lufeng Guan, Shaojuan Jia, Ben Tseng, John Drewe, Sui Xiong Cai

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 133 KB

english, 2005

22

Cytotoxic activities of chitosan nanoparticles and copper-loaded nanoparticles

Lifeng Qi, Zirong Xu, Xia Jiang, Yan Li, Minqi Wang

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 98 KB

english, 2005

23

Interaction of dopamine and acetylcholine with an amphiphilic resorcinarene receptor in aqueous micelle system

Makoto Demura, Tsutomu Yoshida, Takatsugu Hirokawa, Yasuhiro Kumaki, Tomoyasu Aizawa, Katsutoshi Nitta, Isván Bitter, Klára Tóth

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 246 KB

english, 2005

24

Ab initio studies of the properties of intracellular thiols ergothioneine and ovothiol

Christine E. Hand, Nicholas J. Taylor, John F. Honek

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 131 KB

english, 2005

25

(R)-2-(4-Phenylbutyl)dihydrobenzofuran derivatives as melatoninergic agents

Li-Qiang Sun, Katherine Takaki, Jie Chen, Stephen Bertenshaw, Lawrence Iben, Cathy D. Mahle, Elaine Ryan, Dedong Wu, Qi Gao, Cen Xu

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 160 KB

english, 2005

26

The synthesis of substituted bipiperidine amide compounds as CCR3 antagonists

Pauline C. Ting, Joe F. Lee, Jie Wu, Shelby P. Umland, Robert Aslanian, Jianhua Cao, Youhao Dong, Charles G. Garlisi, Eric J. Gilbert, Ying Huang, James Jakway, Joseph Kelly, Zhidan Liu, Stuart McComb

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 124 KB

english, 2005

27

Utilization of a nitrobenzoxadiazole (NBD) fluorophore in the design of a Grb2 SH2 domain-binding peptide mimetic

Zhen-Dan Shi, Rajeshri G. Karki, Shinya Oishi, Karen M. Worthy, Lakshman K. Bindu, Pathirage G. Dharmawardana, Marc C. Nicklaus, Donald P. Bottaro, Robert J. Fisher, Terrence R. Burke Jr.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 208 KB

english, 2005

28

Tetrahedron prize for creativity in organic chemistry for 2004

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 209 KB

english, 2005

29

The discovery and synthesis of novel adenosine receptor (A2A) antagonists

Julius J. Matasi, John P. Caldwell, Jinsong Hao, Bernard Neustadt, Leyla Arik, Carolyn J. Foster, Jean Lachowicz, Deen B. Tulshian

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 122 KB

english, 2005

30

Synthesis and evaluation of pyrazolidine derivatives as dipeptidyl peptidase IV (DP-IV) inhibitors

Jin Hee Ahn, Jin Ah Kim, Hye-Min Kim, Hyuk-Man Kwon, Sun-Chul Huh, Sang Dal Rhee, Kwang Rok Kim, Sung-Don Yang, Sung-Dae Park, Jae Mok Lee, Sung Soo Kim, Hyae Gyeong Cheon

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 117 KB

english, 2005

31

Chiral polyamines from reduction of polypeptides: asymmetric pyridoxamine-mediated transaminations

Wenjun Zhou, Nancy Yerkes, Jason J. Chruma, Lei Liu, Ronald Breslow

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 143 KB

english, 2005

32

cis-6-Oxo-hexahydro-2-oxa-1,4-diazapentalene and cis-6-oxo-hexahydropyrrolo[3,2-c]pyrazole based scaffolds: design rationale, synthesis and cysteinyl proteinase inhibition

Yikang Wang, Alex Benn, Nick Flinn, Tracy Monk, Manoj Ramjee, John Watts, Martin Quibell

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 145 KB

english, 2005

33

Functionalized dendrimers as endotoxin sponges

Jens R. Cromer, Stewart J. Wood, Kelly A. Miller, Thuan Nguyen, Sunil A. David

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 154 KB

english, 2005

34

Synthesis and biological activity of new 5-O-sugar modified ketolide and 2-fluoro-ketolide antibiotics

Chang-Hsing Liang, Sulan Yao, Yu-Hung Chiu, Po Yee Leung, Nicole Robert, Jaime Seddon, Pam Sears, Chan-Kou Hwang, Yoshi Ichikawa, Alex Romero

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 142 KB

english, 2005

35

Interstrand photocrosslinking of DNA via p-carbamoylvinyl phenol nucleoside

Yoshinaga Yoshimura, Yoshiaki Ito, Kenzo Fujimoto

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 135 KB

english, 2005

36

Effects of suberoylanilide hydroxamic acid and trichostatin A on induction of cytochrome P450 enzymes and benzo[a]pyrene DNA adduct formation in human cells

Louisa A. Hooven, Brinda Mahadevan, Channa Keshava, Christopher Johns, Cliff Pereira, Dhimant Desai, Shantu Amin, Ainsley Weston, William M. Baird

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 132 KB

english, 2005

37

Synthesis and radiopharmacological evaluation of 2′-(4-fluorophenyl)-21-[18F]fluoro-20-oxo-11β,17α-dihydroxy-pregn-4-eno[3,2-c]pyrazole as potential glucocorticoid receptor ligand for positron emission tomography (PET)

Frank Wüst, Torsten Kniess, Marion Kretzschmar, Ralf Bergmann

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 183 KB

english, 2005

38

Biaryls and heterobiaryls as α-glucosidase and protein tyrosine phosphatase inhibitors

Ashoke Sharon, Ramendra Pratap, Brajendra Tripathi, A.K. Srivastava, P.R. Maulik, Vishnu Ji Ram

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 106 KB

english, 2005

39

Amino acid conjugates as κ opioid receptor agonists

Virendra Kumar, Deqi Guo, Jeffrey D. Daubert, Joel A. Cassel, Robert N. DeHaven, Erik Mansson, Diane L. DeHaven-Hudkins, Alan L. Maycock

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 115 KB

english, 2005

40

Design of dantrolene-derived probes for radioisotope-free photoaffinity labeling of proteins involved in the physiological Ca2+ release from sarcoplasmic reticulum of skeletal muscle

Takamitsu Hosoya, Toshiyuki Hiramatsu, Takaaki Ikemoto, Hiroshi Aoyama, Tatsuro Ohmae, Makoto Endo, Masaaki Suzuki

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 219 KB

english, 2005

41

Editorial board

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

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PDF, 322 KB

english, 2005

42

Graphical contents list

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 787 KB

english, 2005

43

Contributors to this issue

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

File:

PDF, 191 KB

2005

44

Instructions to contributors

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 71 KB

english, 2005

45

(E)-Phenyl- and -heteroaryl-substituted O-benzoyl-(or acyl)oximes as lipoprotein-associated phospholipase A2 inhibitors

Tae-Sook Jeong, Mi Jeong Kim, Hana Yu, Kyung Soon Kim, Joong-Kwon Choi, Sung-Soo Kim, Woo Song Lee

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 103 KB

english, 2005

46

Benzothiophenes containing a piperazine side chain as selective ligands for the estrogen receptor α and their bioactivities in vivo

Chunhao Yang, Guangyu Xu, Jia Li, Xihan Wu, Bo Liu, Xueming Yan, Mingwei Wang, Yuyuan Xie

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 147 KB

english, 2005

47

Synthesis and activity of 4,5-diarylimidazoles as human CB1 receptor inverse agonists

Christopher W. Plummer, Paul E. Finke, Sander G. Mills, Junying Wang, Xinchun Tong, George A. Doss, Tung M. Fong, Julie Z. Lao, Marie-Therese Schaeffer, Jing Chen, Chun-Pyn Shen, D. Sloan Stribling, L

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 216 KB

english, 2005

48

Synthesis and SAR of 4-(3-hydroxyphenylamino)pyrrolo[2,1-f][1,2,4]triazine based VEGFR-2 kinase inhibitors

Robert M. Borzilleri, Zhen-wei Cai, Christopher Ellis, Joseph Fargnoli, Aberra Fura, Tracy Gerhardt, Bindu Goyal, John T. Hunt, Steven Mortillo, Ligang Qian, John Tokarski, Viral Vyas, Barri Wautlet,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 148 KB

english, 2005

49

Discovery and SAR of new benzazepines as potent and selective 5-HT2C receptor agonists for the treatment of obesity

Brian M. Smith, Jeffrey M. Smith, James H. Tsai, Jeffrey A. Schultz, Charles A. Gilson, Scott A. Estrada, Rita R. Chen, Douglas M. Park, Emily B. Prieto, Charlemagne S. Gallardo, Dipanjan Sengupta, Wi

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 119 KB

english, 2005

50

Novel jadomycins: incorporation of non-natural and natural amino acids

David L. Jakeman, Spring Farrell, Wendy Young, René J. Doucet, Shannon C. Timmons

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 169 KB

english, 2005

51

Crystal structures of human HSP90α-complexed with dihydroxyphenylpyrazoles

Andreas Kreusch, Shulin Han, Achim Brinker, Vicki Zhou, Ha-soon Choi, Yun He, Scott A. Lesley, Jeremy Caldwell, Xiang-ju Gu

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 355 KB

english, 2005

52

Synthesis and in vitro antitrypanosomal activity of novel Nifurtimox analogues

Rocío Pozas, Javier Carballo, Clementina Castro, Julieta Rubio

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 112 KB

english, 2005

53

Efficient synthesis of bicyclic oxazolino- and thiazolino[3,2-c]pyrimidine-5,7-diones and its application to the synthesis of GnRH antagonists

Joseph Pontillo, Chen Chen

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 149 KB

english, 2005

54

Design, synthesis and biological evaluation of novel bicyclic β-lactams as potential antimalarials

Manisha Nivsarkar, D. Thavaselvam, S. Prasanna, Mamta Sharma, M.P. Kaushik

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 99 KB

english, 2005

55

Novel and orally bioavailable inducible nitric oxide synthase inhibitors: synthesis and evaluation of optically active 4,5-dialkyl-2-iminoselenazolidine derivatives

Shigeo Ueda, Hideo Terauchi, Kenji Suzuki, Akihiro Yano, Masashi Matsumoto, Taeko Kubo, Hisao Minato, Yukiyo Arai, Jun-ichi Tsuji, Nobuhide Watanabe

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 159 KB

english, 2005

56

Benzodipyrazoles: a new class of potent CDK2 inhibitors

Roberto D’Alessio, Alberto Bargiotti, Suzanne Metz, M. Gabriella Brasca, Alexander Cameron, Antonella Ermoli, Aurelio Marsiglio, Paolo Polucci, Fulvia Roletto, Marcellino Tibolla, Michael L. Vazquez,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 215 KB

english, 2005

57

N-i-Propoxy-N-biphenylsulfonylaminobutylhydroxamic acids as potent and selective inhibitors of MMP-2 and MT1-MMP

Armando Rossello, Elisa Nuti, Paolo Carelli, Elisabetta Orlandini, Marco Macchia, Susanna Nencetti, Maurizio Zandomeneghi, Federica Balzano, Gloria Uccello Barretta, Adriana Albini, Roberto Benelli, G

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 191 KB

english, 2005

58

Identification of an agonist ligand for estrogen-related receptors ERRβ/γ

Donna D. Yu, Barry Marc Forman

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 108 KB

english, 2005