Volume 16; Issue 19

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Bioorganic & Medicinal Chemistry Letters
Volume 16; Issue 19

Bioorganic & Medicinal Chemistry Letters

Volume 16; Issue 19

1

Kinase-mediated trapping of bi-functional conjugates of paclitaxel or vinblastine with thymidine in cancer cells

Simon E. Aspland, Carlo Ballatore, Rosario Castillo, Joel Desharnais, Trisha Eustaquio, Philip Goelet, Zijian Guo, Qing Li, David Nelson, Chengzao Sun, Angelo J. Castellino, Michael J. Newman

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 171 KB

english, 2006

2

New, potent P1/P2-morpholinone-based HIV-protease inhibitors

Wieslaw M. Kazmierski, Eric Furfine, Andrew Spaltenstein, Lois L. Wright

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 141 KB

english, 2006

3

Conjugated indole-imidazole derivatives displaying cytotoxicity against multidrug resistant cancer cell lines

David A. James, Keizo Koya, Hao Li, Shoujun Chen, Zhiqiang Xia, Weiwen Ying, Yaming Wu, Lijun Sun

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 132 KB

english, 2006

4

Carbonic anhydrase activators: The first X-ray crystallographic study of an adduct of isoform I

Claudia Temperini, Andrea Scozzafava, Claudiu T. Supuran

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 392 KB

english, 2006

5

Development of a novel albumin-binding prodrug that is cleaved by urokinase-type-plasminogen activator (uPA)

Da-Eun Chung, Felix Kratz

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 204 KB

english, 2006

6

Novel tricyclic azepine derivatives: Biological evaluation of pyrimido[4,5-b]-1,4-benzoxazepines, thiazepines, and diazepines as inhibitors of the epidermal growth factor receptor tyrosine kinase

Leon Smith II, Wai C. Wong, Alexander S. Kiselyov, Sabina Burdzovic-Wizemann, Yunyu Mao, Yongjiang Xu, Matthew A.J. Duncton, Ki Kim, Evgueni L. Piatnitski, Jacqueline F. Doody, Ying Wang, Robin L. Ros

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 137 KB

english, 2006

7

Synthesis and SAR of arylaminoethyl amides as noncovalent inhibitors of cathepsin S: P3 cyclic ethers

David C. Tully, Hong Liu, Arnab K. Chatterjee, Phil B. Alper, Robert Epple, Jennifer A. Williams, Michael J. Roberts, David H. Woodmansee, Brian T. Masick, Christine Tumanut, Jun Li, Glen Spraggon, Mi

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 185 KB

english, 2006

8

A novel class of AMPA receptor allosteric modulators. Part 1: Design, synthesis, and SAR of 3-aryl-4-cyano-5-substituted-heteroaryl-2-carboxylic acid derivatives

Maria-Carmen Fernandez, Ana Castaño, Esteban Dominguez, Ana Escribano, Delu Jiang, Alma Jimenez, Eric Hong, William J. Hornback, Eric S. Nisenbaum, Nancy Rankl, Eric Tromiczak, Grant Vaught, Hamideh Z

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 230 KB

english, 2006

9

Synthesis and neuroprotective effects of serofendic acid analogues

Taro Terauchi, Takashi Doko, Masahiro Yonaga, Akiharu Kajiwara, Tetsuhiro Niidome, Ryota Taguchi, Toshiaki Kume, Akinori Akaike, Hachiro Sugimoto

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 239 KB

english, 2006

10

Structurally diverse 5-substituted pyrimidine nucleosides as inhibitors of Leishmania donovani promastigotes in vitro

Paul F. Torrence, Xuesen Fan, Xinying Zhang, Philippe M. Loiseau

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 135 KB

english, 2006

11

Des-keto lobeline analogs with increased potency and selectivity at dopamine and serotonin transporters

Guangrong Zheng, David B. Horton, Agripina G. Deaciuc, Linda P. Dwoskin, Peter A. Crooks

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 147 KB

english, 2006

12

Stereospecificity in hydroxyl radical scavenging activities of four ginsenosides produced by heat processing

Ki Sung Kang, Hyun Young Kim, Noriko Yamabe, Takako Yokozawa

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 286 KB

english, 2006

13

Antitumour properties of fluorinated benzothiazole-substituted hydroxycyclohexa-2,5-dienones (‘quinols’)

Cedric J. Lion, Charles S. Matthews, Geoffrey Wells, Tracey D. Bradshaw, Malcolm F.G. Stevens, Andrew D. Westwell

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 126 KB

english, 2006

14

Morpholin-2-one derivatives as novel selective T-type Ca2+ channel blockers

Il Whea Ku, Sangwon Cho, Munikumar Reddy Doddareddy, Min Seok Jang, Gyochang Keum, Jung-Ha Lee, Bong Young Chung, Youseung Kim, Hyewhon Rhim, Soon Bang Kang

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 274 KB

english, 2006

15

Homo-cysteinyl peptide inhibitors of the L1 metallo-β-lactamase, and SAR as determined by combinatorial library synthesis

Qin Sun, Andy Law, Michael W. Crowder, H. Mario Geysen

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 185 KB

english, 2006

16

Selectively guanidinylated derivatives of neamine. Syntheses and inhibition of anthrax lethal factor protease

Guan-Sheng Jiao, Ondrej Simo, Melissa Nagata, Sean O’Malley, Thomas Hemscheidt, Lynne Cregar, Sherri Z. Millis, Mark E. Goldman, Cho Tang

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 178 KB

english, 2006

17

Design and synthesis of substituted quinolines as novel and selective melanin concentrating hormone antagonists as anti-obesity agents

Namal C. Warshakoon, Justin Sheville, Ritu Tiku Bhatt, Wei Ji, Jose L. Mendez-Andino, Kenneth M. Meyers, Nick Kim, John A. Wos, Chrissy Mitchell, Jennifer L. Paris, Beth B. Pinney, Ofer Reizes, X. Eri

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 142 KB

english, 2006

18

From arylureas to biarylamides to aminoquinazolines: Discovery of a novel, potent TRPV1 antagonist

Xiaozhang Zheng, Kevin J. Hodgetts, Harry Brielmann, Alan Hutchison, Frank Burkamp, A. Brian Jones, Peter Blurton, Robert Clarkson, Jayaraman Chandrasekhar, Rajagopal Bakthavatchalam, Stéphane De Lomb

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 136 KB

english, 2006

19

A novel class of positive allosteric modulators of AMPA receptors: Design, synthesis, and structure–activity relationships of 3-biphenyl-4-yl-4-cyano-5-ethyl-1-methyl-1H-pyrrole-2-carboxylic acid, LY2059346

Hamideh Zarrinmayeh, Eric Tromiczak, Dennis M. Zimmerman, Nancy Rankl, Ken H. Ho, Esteban Dominguez, Ana Castaño, Ana Escribano, Carmen Fernandez, Alma Jimenez, William J. Hornback, Eric S. Nisenbaum

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 130 KB

english, 2006

20

Synthesis and monoamine transporter affinity of 2β-carbomethoxy-3β-(4′-p-substituted phenyl)-piperidine analogs of cocaine

Frederic Bois, Ronald M. Baldwin, Nora S. Kula, Ross J. Baldessarini, M. Al Tikriti, Robert B. Innis, Gilles D. Tamagnan

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 126 KB

english, 2006

21

Mimicking the biological activity of diazobenzo[b]fluorene natural products with electronically tuned diazofluorene analogs

Wei Zeng, T. Eric Ballard, Alexander G. Tkachenko, Virginia A. Burns, Daniel L. Feldheim, Christian Melander

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 182 KB

english, 2006

22

Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure

Nobuhiko Kawanishi, Tetsuya Sugimoto, Jun Shibata, Kaori Nakamura, Kouta Masutani, Mari Ikuta, Hiroshi Hirai

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 184 KB

english, 2006

23

Synthesis of 3H-spiro[benzofuran-2,1′-cyclohexane] derivatives from naturally occurring filifolinol and their classical complement pathway inhibitory activity

Mariana Useglio, Patricia M. Castellano, María A. Operto, René Torres, Teodoro S. Kaufman

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 151 KB

english, 2006

24

Arylaminoethyl carbamates as a novel series of potent and selective cathepsin S inhibitors

David C. Tully, Hong Liu, Arnab K. Chatterjee, Phil B. Alper, Jennifer A. Williams, Michael J. Roberts, Daniel Mutnick, David H. Woodmansee, Thomas Hollenbeck, Perry Gordon, Jonathan Chang, Tove Tuntl

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 157 KB

english, 2006

25

The molecular basis for the selection of captopril cis and trans conformations by angiotensin I converting enzyme

Andreas G. Tzakos, Nawazish Naqvi, Konstantinos Comporozos, Roberta Pierattelli, Vassiliki Theodorou, Ahsan Husain, Ioannis P. Gerothanassis

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 343 KB

english, 2006

26

Pyrrolidine bis-cyclic guanidines with antimicrobial activity against drug-resistant Gram-positive pathogens identified from a mixture-based combinatorial library

Mary E. Hensler, Gregory Bernstein, Victor Nizet, Adel Nefzi

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 328 KB

english, 2006

27

Selectivity in DNA interstrand-stacking

Simon M. Langenegger, Robert Häner

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 183 KB

english, 2006

28

Synthesis and in vitro biological evaluation of aryl boronic acids as potential inhibitors of factor XIa

Tsvetelina I. Lazarova, Lei Jin, Michael Rynkiewicz, Joan C. Gorga, Frank Bibbins, Harold V. Meyers, Robert Babine, James Strickler

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 325 KB

english, 2006

29

Synthesis, radiolabeling, and in vivo evaluation of an 18F-labeled isatin analog for imaging caspase-3 activation in apoptosis

Dong Zhou, Wenhua Chu, Justin Rothfuss, Chenbo Zeng, Jinbin Xu, Lynne Jones, Michael J. Welch, Robert H. Mach

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 213 KB

english, 2006

30

Syntheses of triazole-modified zanamivir analogues via click chemistry and anti-AIV activities

Jian Li, Mingyue Zheng, Wei Tang, Pei-Lan He, Weiliang Zhu, Tianxian Li, Jian-Ping Zuo, Hong Liu, Hualiang Jiang

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 265 KB

english, 2006

31

Site-Selective DNA cleavage by a novel complex of copper-conjugate of Phen and polyamide containing N-methylimidazole rings

Dan Liu, Jiang Zhou, Huihui Li, Bo Zheng, Gu Yuan

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 172 KB

english, 2006

32

Novel benzimidazole-based MCH R1 antagonists

Andrew J. Carpenter, Kamal A. Al-Barazanji, Kevin K. Barvian, Michael J. Bishop, Christy S. Britt, Joel P. Cooper, Aaron S. Goetz, Mary K. Grizzle, Donald L. Hertzog, Diane M. Ignar, Ronda O. Morgan,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 164 KB

english, 2006

33

Identification of potent agonists of photoreceptor-specific nuclear receptor (NR2E3) and preparation of a radioligand

Scott E. Wolkenberg, Zhijian Zhao, Marianna Kapitskaya, Andrea L. Webber, Konstantin Petrukhin, Yui Sing Tang, Dennis C. Dean, George D. Hartman, Craig W. Lindsley

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 133 KB

english, 2006

34

Improved replicon cellular activity of non-nucleoside allosteric inhibitors of HCV NS5B polymerase: From benzimidazole to indole scaffolds

Pierre L. Beaulieu, James Gillard, Darren Bykowski, Christian Brochu, Nathalie Dansereau, Jean-Simon Duceppe, Bruno Haché, Araz Jakalian, Lisette Lagacé, Steven LaPlante, Ginette McKercher, Elaine Mor

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 186 KB

english, 2006

35

Editorial Board

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 3.38 MB

english, 2006

36

Graphical contents list

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 1013 KB

english, 2006

37

Instructions to contributors

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 29 KB

english, 2006

38

Synthesis and evaluation of anilinohexafluoroisopropanols as activators/modulators of LXRα and β

Narendra Panday, Jörg Benz, Denise Blum-Kaelin, Vanessa Bourgeaux, Henrietta Dehmlow, Peter Hartman, Bernd Kuhn, Hassen Ratni, Xavier Warot, Matthew B. Wright

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 210 KB

english, 2006

39

Convenient synthesis of 3- and 6-deoxy-d-myo-inositol phosphate analogues from (+)-epi- and (−)-vibo-quercitols

Seiichiro Ogawa, Yoji Tezuka

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 193 KB

english, 2006

40

Preparation of 1-(3-aminobenzo[d]isoxazol-5-yl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective, and efficacious inhibitors of coagulation factor Xa

Yun-Long Li, John M. Fevig, Joseph Cacciola, Joseph Buriak Jr., Karen A. Rossi, Janan Jona, Robert M. Knabb, Joseph M. Luettgen, Pancras C. Wong, Stephen A. Bai, Ruth R. Wexler, Patrick Y.S. Lam

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 180 KB

english, 2006

41

Synthesis of 16-mercaptohexadecylphosphocholine, a miltefosine analog with leishmanicidal activity

Valentín Hornillos, José María Saugar, Beatriz G. de la Torre, David Andreu, Luis Rivas, A. Ulises Acuña, Francisco Amat-Guerri

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 137 KB

english, 2006

42

Synthesis and SAR of conformationally restricted inhibitors of soluble epoxide hydrolase

Paul D. Jones, Hsing-Ju Tsai, Zung N. Do, Christophe Morisseau, Bruce D. Hammock

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 194 KB

english, 2006

43

Inhibition of HIV-1 integrase activity by synthetic peptides derived from the HIV-1 HXB2 Pol region of the viral genome

Zahrah Zawahir, Nouri Neamati

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 217 KB

english, 2006

44

Search of antitubercular activities in tetrahydroacridines: Synthesis and biological evaluation

R.P. Tripathi, S.S. Verma, Jyoti Pandey, K.C. Agarwal, Vinita Chaturvedi, Y.K. Manju, A.K. Srivastva, A. Gaikwad, S. Sinha

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 122 KB

english, 2006

45

Enhanced reactivity of amino-modified oligonucleotides by insertion of aromatic residue

Naoshi Kojima, Maiko Sugino, Akiko Mikami, Ken Nonaka, Yumi Fujinawa, Isamu Muto, Kenichi Matsubara, Eiko Ohtsuka, Yasuo Komatsu

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 262 KB

english, 2006

46

Protein microarrays to study carbohydrate-recognition events

Myung-ryul Lee, Sungjin Park, Injae Shin

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 173 KB

english, 2006

47

Design and regioselective synthesis of a new generation of targeted chemotherapeutics. Part 1: EC145, a folic acid conjugate of desacetylvinblastine monohydrazide

Iontcho R. Vlahov, Hari Krishna R. Santhapuram, Paul J. Kleindl, Stephen J. Howard, Katheryn M. Stanford, Christopher P. Leamon

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 260 KB

english, 2006

48

Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: Increased receptor specificity and in vivo activity

Karsten Schnatbaum, Elsa Locardi, Dirk Scharn, Uwe Richter, Heiko Hawlisch, Jochen Knolle, Thomas Polakowski

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 168 KB

english, 2006

49

Solid-phase synthesis and structure–activity relationships of novel biarylethers as melanin-concentrating hormone receptor-1 antagonists

Vu Ma, Anthony W. Bannon, Jamie Baumgartner, Clarence Hale, Faye Hsieh, Christopher Hulme, Kirk Rorrer, John Salon, Carlo van Staden, Paul Tempest

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 178 KB

english, 2006

50

Cluster analysis and two-dimensional quantitative structure–activity relationship (2D-QSAR) of Pseudomonas aeruginosa deacetylase LpxC inhibitors

Rameshwar U. Kadam, Nilanjan Roy

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 208 KB

english, 2006

51

Benzodiazepine calcitonin gene-related peptide (CGRP) receptor antagonists: Optimization of the 4-substituted piperidine

Christopher S. Burgey, Craig A. Stump, Diem N. Nguyen, James Z. Deng, Amy G. Quigley, Beth R. Norton, Ian M. Bell, Scott D. Mosser, Christopher A. Salvatore, Ruth Z. Rutledge, Stefanie A. Kane, Kennet

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 137 KB

english, 2006

52

Growth inhibition of human cancer cells in vitro by T-type calcium channel blockers

Jae Yeol Lee, Seong Jun Park, Sung Jun Park, Min Joo Lee, Hyewhon Rhim, Seon Hee Seo, Ki-Sun Kim

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 116 KB

english, 2006

53

Synthesis, structure, and bioactivity of N′-substituted benzylidene-3,4,5-trimethoxybenzohydrazide and 3-acetyl-2-substituted phenyl-5-(3,4,5-trimethoxyphenyl)-2,3-dihydro-1,3,4-oxadiazole derivatives

Linhong Jin, Jiang Chen, Baoan Song, Zhuo Chen, Song Yang, Qianzhu Li, Deyu Hu, Ruiqing Xu

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 150 KB

english, 2006

54

Synthesis and biological evaluation of benzamides and benzamidines as selective inhibitors of VEGFR tyrosine kinases

Hiroyuki Nakamura, Yusuke Sasaki, Masaharu Uno, Tomohiro Yoshikawa, Toru Asano, Hyun Seung Ban, Hidesuke Fukazawa, Masabumi Shibuya, Yoshimasa Uehara

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 169 KB

english, 2006

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