Volume 20; Issue 4

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Bioorganic & Medicinal Chemistry Letters
Volume 20; Issue 4

Bioorganic & Medicinal Chemistry Letters

Volume 20; Issue 4

1

Synthesis of bisboron compounds and their strong inhibitory activity on store-operated calcium entry

Akinobu Z. Suzuki, Shoichiro Ozaki, Jun-Ichi Goto, Katsuhiko Mikoshiba

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 348 KB

english, 2010

2

Chemoenzymatic synthesis of 1-deaza-pyridoxal 5′-phosphate

Wait R. Griswold, Michael D. Toney

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 172 KB

english, 2010

3

N-Heterocyclic derived M1 positive allosteric modulators

Scott D. Kuduk, Christina N. Di Marco, Victoria Cofre, Daniel R. Pitts, William J. Ray, Lei Ma, Marion Wittmann, Lone Veng, Matthew A. Seager, Kenneth Koeplinger, Charles D. Thompson, George D. Hartma

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 1.60 MB

english, 2010

4

Synthesis and structure–activity relationship of botryllamides that block the ABCG2 multidrug transporter

Kentaro Takada, Nobutaka Imamura, Kirk R. Gustafson, Curtis J. Henrich

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 747 KB

english, 2010

5

New potential antitumor compounds from the plant Aristolochia manshuriensis as inhibitors of the CDK2 enzyme

Vinod R. Hegde, Scott Borges, Mahesh Patel, Pradip R. Das, Bonnie Wu, Vincent P. Gullo, Tze-Ming Chan

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 186 KB

english, 2010

6

A fluorescent redox sensor with tuneable oxidation potential

Radoslaw M. Kierat, Birgit M.B. Thaler, Roland Krämer

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 248 KB

english, 2010

7

Boron-containing phenoxyacetanilide derivatives as hypoxia-inducible factor (HIF)-1α inhibitors

Kazuki Shimizu, Minako Maruyama, Yuka Yasui, Hidemitsu Minegishi, Hyun Seung Ban, Hiroyuki Nakamura

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 525 KB

english, 2010

8

Furo[2,3-b]pyridine-based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation. Part 1

John S. Debenham, Christina B. Madsen-Duggan, Richard B. Toupence, Thomas F. Walsh, Junying Wang, Xinchun Tong, Sanjeev Kumar, Julie Lao, Tung M. Fong, Jing Chen Xiao, Cathy R.-R.C. Huang, Chun-Pyn Sh

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 482 KB

english, 2010

9

Pyrrolidine amides of pyrazolodihydropyrimidines as potent and selective KV1.5 blockers

John Lloyd, Heather J. Finlay, Wayne Vacarro, Tram Hyunh, Alexander Kover, Rao Bhandaru, Lin Yan, Karnail Atwal, Mary Lee Conder, Tonya Jenkins-West, Hong Shi, Christine Huang, Danshi Li, Huabin Sun,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 640 KB

english, 2010

10

Pyrazolopyrimidines as highly potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): Optimization of the 1-substituent

Kevin J. Curran, Jeroen C. Verheijen, Joshua Kaplan, David J. Richard, Lourdes Toral-Barza, Irwin Hollander, Judy Lucas, Semiramis Ayral-Kaloustian, Ker Yu, Arie Zask

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 1.16 MB

english, 2010

11

Discovery of olodaterol, a novel inhaled β2-adrenoceptor agonist with a 24 h bronchodilatory efficacy

Thierry Bouyssou, Christoph Hoenke, Klaus Rudolf, Philipp Lustenberger, Sabine Pestel, Peter Sieger, Ralf Lotz, Claudia Heine, Frank H. Büttner, Andreas Schnapp, Ingo Konetzki

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 301 KB

english, 2010

12

Novel bis-2,2,6,6-tetramethylpiperidine (bis-TMP) and bis-mecamylamine antagonists at neuronal nicotinic receptors mediating nicotine-evoked dopamine release

Zhenfa Zhang, Marharyta Pivavarchyk, Karunai Leela Subramanian, A. Gabriela Deaciuc, Linda P. Dwoskin, Peter A. Crooks

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 455 KB

english, 2010

13

Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors

G.D. Kishore Kumar, Gustavo E. Chavarria, Amanda K. Charlton-Sevcik, Wara M. Arispe, Matthew T. MacDonough, Tracy E. Strecker, Shen-En Chen, Bronwyn G. Siim, David J. Chaplin, Mary Lynn Trawick, Kevin

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 566 KB

english, 2010

14

Synthesis and structure–activity relationship of substitutions at the C-1 position of Δ9-tetrahydrocannabinol

David Burdick, Russell DeOrazio, Peter Guzzo, Alicia Habershaw, Mark Helle, Bernard Paul, Mark Wolf

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 563 KB

english, 2010

15

RNA-hydrolyzing activity of human serum albumin and its recombinant analogue

Yulia V. Gerasimova, Tatyana V. Bobik, Natalya A. Ponomarenko, Makhmut M. Shakirov, Marina A. Zenkova, Nikolai V. Tamkovich, Tatyana V. Popova, Dmitry G. Knorre, Tatyana S. Godovikova

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 551 KB

english, 2010

16

Synthesis and discovery of 2,3-dihydro-3,8-diphenylbenzo[1,4]oxazines as a novel class of potent cholesteryl ester transfer protein inhibitors

Aihua Wang, Catherine P. Prouty, Patricia D. Pelton, Maria Yong, Keith T. Demarest, William V. Murray, Gee-Hong Kuo

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 518 KB

english, 2010

17

Interaction of heparin with cationic molecular probes: Probe charge is a major determinant of binding stoichiometry and affinity

Helga Szelke, Sarah Schübel, Job Harenberg, Roland Krämer

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 246 KB

english, 2010

18

Synthesis and biological activities of novel indole derivatives as potent and selective PPARγ modulators

Yann Lamotte, Paul Martres, Nicolas Faucher, Alain Laroze, Didier Grillot, Nicolas Ancellin, Yannick Saintillan, Véronique Beneton, Robert T. Gampe Jr.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 544 KB

english, 2010

19

Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors

Hiroki Nishii, Takashi Chiba, Kenji Morikami, Takaaki A. Fukami, Hiroshi Sakamoto, Kwangseok Ko, Hiroshi Koyano

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 728 KB

english, 2010

20

Part II: Piperazinyl-glutamate-pyridines as potent orally bioavailable P2Y12 antagonists for inhibition of platelet aggregation

John J. Parlow, Mary W. Burney, Brenda L. Case, Thomas J. Girard, Kerri A. Hall, Peter K. Harris, Ronald R. Hiebsch, Rita M. Huff, Rhonda M. Lachance, Deborah A. Mischke, Stephen R. Rapp, Rhonda S. Wo

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 1.49 MB

english, 2010

21

Structure–activity relationships amongst 4-position quinoline methanol antimalarials that inhibit the growth of drug sensitive and resistant strains of Plasmodium falciparum

Erin Milner, William McCalmont, Jayendra Bhonsle, Diana Caridha, Dustin Carroll, Sean Gardner, Lucia Gerena, Montip Gettayacamin, Charlotte Lanteri, ThuLan Luong, Victor Melendez, Jay Moon, Norma Ronc

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 283 KB

english, 2010

22

Synthesis and structure–activity relationships of a series of 3-aryl-4-isoxazolecarboxamides as a new class of TGR5 agonists

Brian W. Budzik, Karen A. Evans, David D. Wisnoski, Jian Jin, Ralph A. Rivero, George R. Szewczyk, Channa Jayawickreme, David L. Moncol, Hongshi Yu

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 633 KB

english, 2010

23

Design and study of peptide-based inhibitors of amylin cytotoxicity

Karen Muthusamy, Per I. Arvidsson, Patrick Govender, Hendrik G. Kruger, Glenn E.M. Maguire, Thavendran Govender

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 343 KB

english, 2010

24

Synthesis and in vitro evaluation of bisphosphonated glycopeptide prodrugs for the treatment of osteomyelitis

Kelly S.E. Tanaka, Evelyne Dietrich, Stéphane Ciblat, Claude Métayer, Francis F. Arhin, Ingrid Sarmiento, Gregory Moeck, Thomas R. Parr Jr., Adel Rafai Far

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 458 KB

english, 2010

25

Semi-synthetic aristolactams—inhibitors of CDK2 enzyme

Vinod R. Hegde, Scott Borges, Haiyan Pu, Mahesh Patel, Vincent P. Gullo, Bonnie Wu, Paul Kirschmeier, Michael J. Williams, Vincent Madison, Thierry Fischmann, Tze-Ming Chan

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 321 KB

english, 2010

26

Structure–activity relationships of diphenylpiperazine N-type calcium channel inhibitors

Hassan Pajouhesh, Zhong-Ping Feng, Yanbing Ding, Lingyun Zhang, Hossein Pajouhesh, Jerrie-Lynn Morrison, Francesco Belardetti, Elizabeth Tringham, Eric Simonson, Todd W. Vanderah, Frank Porreca, Geral

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 314 KB

english, 2010

27

Phenyltriazolinones as potent factor Xa inhibitors

Mimi L. Quan, Donald J.P. Pinto, Karen A. Rossi, Steven Sheriff, Richard S. Alexander, Eugene Amparo, Kevin Kish, Robert M. Knabb, Joseph M. Luettgen, Paul Morin, Angela Smallwood, Francis J. Woerner,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 1.17 MB

english, 2010

28

Potent oxadiazole CGRP receptor antagonists for the potential treatment of migraine

Paula L. Nichols, Jonathan Brand, Michael Briggs, Mathilde D’Angeli, Jennifer Farge, Stephen L. Garland, Paul Goldsmith, Rio Hutchings, Ian Kilford, Ho Y. Li, David MacPherson, Fiona Nimmo, Francis Do

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 580 KB

english, 2010

29

Celecoxib analogs possessing a N-(4-nitrooxybutyl)piperidin-4-yl or N-(4-nitrooxybutyl)-1,2,3,6-tetrahydropyridin-4-yl nitric oxide donor moiety: Synthesis, biological evaluation and nitric oxide release studies

Morshed A. Chowdhury, Khaled R.A. Abdellatif, Ying Dong, Gang Yu, Zhangjian Huang, Moshfiqur Rahman, Dipankar Das, Carlos A. Velázquez, Mavanur R. Suresh, Edward E. Knaus

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 282 KB

english, 2010

30

The Privileged Chemical Space Predictor (pcsp): A computer program that identifies privileged chemical space from screens of modularly assembled chemical libraries

Steven J. Seedhouse, Lucas P. Labuda, Matthew D. Disney

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 533 KB

english, 2010

31

Corrigendum to “Design and synthesis of dipeptidyl nitriles as potent, selective, and reversible inhibitors of cathepsin C” [Bioorg. Med. Chem. Lett. 19 (2009) 5392]

Daniel Guay, Christian Beaulieu, Jean-Francois Truchon, T. Jagadeeswar Reddy, Christopher I. Bayly, Robert Zamboni, Nathalie Methot, Joel Rubin, Diane Ethier, M. David Percival

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 101 KB

english, 2010

32

Corrigendum to “Inhibitors of HIV-1 attachment. Part 2: An initial survey of indole substitution patterns” [Bioorg. Med. Chem. Lett. 19 (2009) 1977]

Nicholas A. Meanwell, Owen B. Wallace, Haiquan Fang, Henry Wang, Milind Deshpande, Tao Wang, Zhiwei Yin, Zhongxing Zhang, Bradley C. Pearce, Jennifer James, Kap-Sun Yeung, Zhilei Qiu, J.J. Kim Wright,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 104 KB

english, 2010

33

Corrigendum to “Inhibitors of HIV-1 attachment. Part 3: A preliminary survey of the effect of structural variation of the benzamide moiety on antiviral activity” [Bioorg. Med. Chem. Lett. 19 (2009) 5136]

Nicholas A. Meanwell, Owen B. Wallace, Henry Wang, Milind Deshpande, Bradley C. Pearce, Ashok Trehan, Kap-Sun Yeung, Zhilei Qiu, J.J. Kim Wright, Brett A. Robinson, Yi-Fei Gong, Hwei-Gene Heidi Wang,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 103 KB

english, 2010

34

Corrigendum to “Inhibitors of HIV-1 attachment. Part 4: A study of the effect of piperazine substitution patterns on antiviral potency in the context of indole-based derivatives” [Bioorg. Med. Chem. Lett. 19 (2009) 5140]

Tao Wang, John F. Kadow, Zhongxing Zhang, Zhiwei Yin, Qi Gao, Dedong Wu, Dawn DiGiugno Parker, Zheng Yang, Lisa Zadjura, Brett A. Robinson, Yi-Fei Gong, Timothy P. Spicer, Wade S. Blair, Pei-Yong Shi,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 104 KB

english, 2010

35

Editorial board

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 35 KB

english, 2010

36

Graphical contents list

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 866 KB

english, 2010

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