Volume 17; Issue 3

Bioorganic & Medicinal Chemistry

Volume 17; Issue 3

1

Synthesis and preliminary antibacterial evaluation of simplified thiomarinol analogs

Olivier Marion, Xuri Gao, Sandra Marcus, Dennis G. Hall

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 446 KB

english, 2009

2

Synthesis and screening of a cyclic peptide library: Discovery of small-molecule ligands against human prolactin receptor

Tao Liu, Sang Hoon Joo, Jeffrey L. Voorhees, Charles L. Brooks, Dehua Pei

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 415 KB

english, 2009

3

Site-specific covalent labeling of proteins inside live cells using small molecule probes

Souvik Chattopadhaya, Rajavel Srinivasan, Dawn S.Y. Yeo, Grace Y.J. Chen, Shao Q. Yao

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 335 KB

english, 2009

4

On-bead cyclization in a combinatorial library of 15,625 octapeptides

Viviana S. Fluxa, Jean-Louis Reymond

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 210 KB

english, 2009

5

Substrate optimization for monitoring cathepsin C activity in live cells

Jun Li, H. Michael Petrassi, Christine Tumanut, Brian T. Masick, Christopher Trussell, Jennifer L. Harris

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 284 KB

english, 2009

6

Expanding the repertoire of small molecule transcriptional activation domains

Ryan J. Casey, Jean-Paul Desaulniers, Jonas W. Hojfeldt, Anna K. Mapp

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 289 KB

english, 2009

7

ATP competitive inhibitors of d-alanine–d-alanine ligase based on protein kinase inhibitor scaffolds

Gemma Triola, Stefan Wetzel, Bernhard Ellinger, Marcus A. Koch, Katja Hübel, Daniel Rauh, Herbert Waldmann

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 845 KB

english, 2009

8

Coulombic effects on the traceless Staudinger ligation in water

Annie Tam, Ronald T. Raines

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 233 KB

english, 2009

9

Sidechain-linked inhibitors of HIV-1 protease dimerization

Michael J. Bowman, Jean Chmielewski

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 685 KB

english, 2009

10

A small molecule inhibitor of α4 integrin-dependent cell migration

Jongkook Lee, Jiyong Hong, Tae-Gyu Nam, Eric C. Peters, Anthony P. Orth, Bernhard H. Geierstanger, Lawrence E. Goldfinger, Mark H. Ginsberg, Charles Y. Cho, Peter G. Schultz

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 371 KB

english, 2009

11

Synthesis, penetrability and intracellular targeting of fluorescein-tagged peptoids and peptide–peptoid hybrids

Asier Unciti-Broceta, Franziska Diezmann, Chiung Ying Ou-Yang, Mario Antonio Fara, Mark Bradley

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 869 KB

english, 2009

12

A road less traveled by: Exploring a decade of Ellman chemistry

Anang A. Shelat, R. Kiplin Guy

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 202 KB

english, 2009

13

Evaluation of α,β-unsaturated ketone-based probes for papain-family cysteine proteases

Zhimou Yang, Marko Fonović, Steven H.L. Verhelst, Galia Blum, Matthew Bogyo

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 264 KB

english, 2009

14

β-Turn secondary structure and melanocortin ligands

Erica M. Haslach, Jay W. Schaub, Carrie Haskell-Luevano

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 574 KB

english, 2009

15

High throughput screening of potentially selective MMP-13 exosite inhibitors utilizing a triple-helical FRET substrate

Janelle L. Lauer-Fields, Dmitriy Minond, Peter S. Chase, Pierre E. Baillargeon, S. Adrian Saldanha, Roma Stawikowska, Peter Hodder, Gregg B. Fields

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 903 KB

english, 2009

16

Ranking the selectivity of PubChem screening hits by activity-based protein profiling: MMP13 as a case study

Ryuichiro Nakai, Cleo M. Salisbury, Hugh Rosen, Benjamin F. Cravatt

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 837 KB

english, 2009

17

Using specificity to strategically target proteases

Mark D. Lim, Charles S. Craik

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 370 KB

english, 2009

18

Synthesis and biological evaluation of a library of resveratrol analogues as inhibitors of COX-1, COX-2 and NF-κB

Soo Sung Kang, Muriel Cuendet, Denise C. Endringer, Vicki L. Croy, John M. Pezzuto, Mark A. Lipton

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 274 KB

english, 2009

19

5′-O-Aliphatic and amino acid ester prodrugs of (−)-β-d-(2R,4R)-dioxolane-thymine (DOT): Synthesis, anti-HIV activity, cytotoxicity and stability studies

Yuzeng Liang, Ashoke Sharon, Jason P. Grier, Kimberly L. Rapp, Raymond F. Schinazi, Chung K. Chu

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 291 KB

english, 2009

20

Synthesis of oligodeoxynucleotides incorporating 2-N-carbamoylguanine and evaluation of the hybridization properties

Takeshi Sasami, Yoko Odawara, Akihiro Ohkubo, Mitsuo Sekine, Kohji Seio

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 357 KB

english, 2009

21

Isolation, structure and biological activity of phomafungin, a cyclic lipodepsipeptide from a widespread tropical Phoma sp.

Kithsiri Herath, Guy Harris, Hiranthi Jayasuriya, Deborah Zink, Scott Smith, Francisca Vicente, Gerald Bills, Javier Collado, Antonio González, Bo Jiang, Jennifer Nielsen Kahn, Stefan Galuska, Robert

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 473 KB

english, 2009

22

Structure-based virtual screening for novel inhibitors of the sarco/endoplasmic reticulum calcium ATPase and their experimental evaluation

Joel Deye, Christopher Elam, Michael Lape, Robert Ratliff, Kayla Evans, Stefan Paula

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 495 KB

english, 2009

23

Modification of the furan ring of salvinorin A: Identification of a selective partial agonist at the kappa opioid receptor

Cécile Béguin, Katharine K. Duncan, Thomas A. Munro, Douglas M. Ho, Wei Xu, Lee-Yuan Liu-Chen, William A. Carlezon Jr., Bruce M. Cohen

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 428 KB

english, 2009

24

Bisubstrate Inhibitors of the MYST HATs Esa1 and Tip60

Jiang Wu, Nan Xie, Zhikun Wu, Ying Zhang, Yujun George Zheng

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 266 KB

english, 2009

25

Determination of 1-aryl-4-propylpiperazine pKa values: The substituent on aryl modulates basicity

Enza Lacivita, Marcello Leopoldo, Paola De Giorgio, Francesco Berardi, Roberto Perrone

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 242 KB

english, 2009

26

Novel boronated chlorin e6-based photosensitizers: Synthesis, binding to albumin and antitumour efficacy

Valentina A. Ol’shevskaya, Roza G. Nikitina, Arina N. Savchenko, Marina V. Malshakova, Alexander M. Vinogradov, Galina V. Golovina, Dmitry V. Belykh, Alexander V. Kutchin, Mikhail A. Kaplan, Valery N.

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 289 KB

english, 2009

27

Synthesis and biological evaluation of extraordinarily potent C-10 carba artemisinin dimers against P. falciparum malaria parasites and HL-60 cancer cells

James Chadwick, Amy E. Mercer, B. Kevin Park, Richard Cosstick, Paul M. O’Neill

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 421 KB

english, 2009

28

Structure–activity relationship study on polyglutamine binding peptide QBP1

Kenji Tomita, H. Akiko Popiel, Yoshitaka Nagai, Tatsushi Toda, Yuji Yoshimitsu, Hiroaki Ohno, Shinya Oishi, Nobutaka Fujii

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 149 KB

english, 2009

29

Cooperative alkylation of double-strand human telomere repeat sequences by PI polyamides with 11-base-pair recognition based on a heterotrimeric design

Gengo Kashiwazaki, Toshikazu Bando, Ken-ichi Shinohara, Masafumi Minoshima, Shigeki Nishijima, Hiroshi Sugiyama

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 371 KB

english, 2009

30

Solid-phase parallel synthesis and SAR of 4-amidofuran-3-one inhibitors of cathepsin S: Effect of sulfonamides P3 substituents on potency and selectivity

Susana Ayesa, Charlotta Lindquist, Tatiana Agback, Kurt Benkestock, Björn Classon, Ian Henderson, Ellen Hewitt, Katarina Jansson, Anders Kallin, Dave Sheppard, Bertil Samuelsson

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 560 KB

english, 2009

31

Towards Gram-negative antivirulence drugs: New inhibitors of HldE kinase

Nicolas Desroy, François Moreau, Sophia Briet, Géraldine Le Fralliec, Stephanie Floquet, Lionel Durant, Vanida Vongsouthi, Vincent Gerusz, Alexis Denis, Sonia Escaich

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 564 KB

english, 2009

32

Novel DNA-directed alkylating agents: Design, synthesis and potent antitumor effect of phenyl N-mustard-9-anilinoacridine conjugates via a carbamate or carbonate linker

Naval Kapuriya, Kalpana Kapuriya, Huajin Dong, Xiuguo Zhang, Ting-Chao Chou, Yu-Ting Chen, Te-Chang Lee, Wen-Chuan Lee, Tung-Hu Tsai, Yogesh Naliapara, Tsann-Long Su

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 642 KB

english, 2009

33

Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference

Claudia Temperini, Alessandro Cecchi, Andrea Scozzafava, Claudiu T. Supuran

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 517 KB

english, 2009

34

Correlation of binding constants and molecular modelling of inhibitors in the active sites of aldose reductase and aldehyde reductase

Vincenzo Carbone, Hai-Tao Zhao, Roland Chung, Satoshi Endo, Akira Hara, Ossama El-Kabbani

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 390 KB

english, 2009

35

New N-substituted 9-azabicyclo[3.3.1]nonan-3α-yl phenylcarbamate analogs as σ2 receptor ligands: Synthesis, in vitro characterization, and evaluation as PET imaging and chemosensitization agents

Wenhua Chu, Jinbin Xu, Dong Zhou, Fanjie Zhang, Lynne A. Jones, Kenneth T. Wheeler, Robert H. Mach

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 291 KB

english, 2009

36

A novel and potent VLA-4 antagonist based on trans-4-substituted cyclohexanecarboxylic acid

Fumihito Muro, Shin Iimura, Yoshiyuki Yoneda, Jun Chiba, Toshiyuki Watanabe, Masaki Setoguchi, Gensuke Takayama, Mika Yokoyama, Tohru Takashi, Atsushi Nakayama, Nobuo Machinaga

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 402 KB

english, 2009

37

Conformational analysis of trimeric maleimide substituted 1,5,9-triazacyclododecane HIV fusion scaffolds

Sarah Remmert, Heather Hollis, Carol A. Parish

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 679 KB

english, 2009

38

Synthesis and biological evaluation of curcuminoid pyrazoles as new therapeutic agents in inflammatory bowel disease: Effect on matrix metalloproteinases

R.M. Claramunt, L. Bouissane, M.P. Cabildo, M.P. Cornago, J. Elguero, A. Radziwon, C. Medina

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 580 KB

english, 2009

39

Isolation, structure elucidation and cytotoxic evaluation of endiandrin B from the Australian rainforest plant Endiandra anthropophagorum

Rohan A. Davis, Emma C. Barnes, James Longden, Vicky M. Avery, Peter C. Healy

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 385 KB

english, 2009

40

Preliminary evaluation of pharmacological properties of some xanthone derivatives

Henryk Marona, Natalia Szkaradek, Anna Rapacz, Barbara Filipek, Małgorzata Dybała, Agata Siwek, Marek Cegła, Edward Szneler

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 1.08 MB

english, 2009

41

Synthesis and cyclooxygenase inhibition of various (aryl-1,2,3-triazole-1-yl)-methanesulfonylphenyl derivatives

Frank Wuest, Xinli Tang, Torsten Kniess, Jens Pietzsch, Mavanur Suresh

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 365 KB

english, 2009

42

Death receptor 5 targeting activity-guided isolation of isoflavones from Millettia brandisiana and Ardisia colorata and evaluation of ability to induce TRAIL-mediated apoptosis

Hiroyuki Kikuchi, Takashi Ohtsuki, Takashi Koyano, Thaworn Kowithayakorn, Toshiyuki Sakai, Masami Ishibashi

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 380 KB

english, 2009

43

Synthesis, structure and antibacterial activity of new 2-(1-(2-(substituted-phenyl)-5-methyloxazol-4-yl)-3-(2-substitued-phenyl)-4,5-dihydro-1H-pyrazol-5-yl)-7-substitued-1,2,3,4-tetrahydroisoquinoline derivatives

Xin-Hua Liu, Jing Zhu, An-na Zhou, Bao-An Song, Hai-Liang Zhu, Lin-Shan bai, Pinaki S. Bhadury, Chun-Xiu Pan

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 225 KB

english, 2009

44

Carbonic anhydrase inhibitors: Inhibition of the β-class enzyme from the yeast Saccharomyces cerevisiae with sulfonamides and sulfamates

Semra Isik, Feray Kockar, Meltem Aydin, Oktay Arslan, Ozen Ozensoy Guler, Alessio Innocenti, Andrea Scozzafava, Claudiu T. Supuran

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 368 KB

english, 2009

45

Synthesis and antitumor activity of novel enediyne-linked pyrrolo[2,1-c][1,4]benzodiazepine hybrids

Wan-Ping Hu, Jium-Jia Liang, Chai-Lin Kao, You-Chiang Chen, Chung-Yu Chen, Feng-Yuan Tsai, Ming-Jung Wu, Long-Sen Chang, Yeh-Long Chen, Jeh-Jeng Wang

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 557 KB

english, 2009

46

Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: A novel, potent and orally active direct inhibitor of factor Xa

Tsutomu Nagata, Toshiharu Yoshino, Noriyasu Haginoya, Kenji Yoshikawa, Masatoshi Nagamochi, Syozo Kobayashi, Satoshi Komoriya, Aki Yokomizo, Ryo Muto, Mitsuhiro Yamaguchi, Ken Osanai, Makoto Suzuki, H

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 549 KB

english, 2009

47

Synthesis of buprestins D, E, F, G and H; structural confirmation and biological testing of acyl glucoses from jewel beetles (Coleoptera: Buprestidae)

Sebastian Ryczek, Konrad Dettner, Carlo Unverzagt

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 235 KB

english, 2009

48

Benzopyridooxathiazepine derivatives as novel potent antimitotic agents

Sebastien Gallet, Nathalie Flouquet, Pascal Carato, Bruno Pfeiffer, Pierre Renard, Stéphane Léonce, Alain Pierré, Pascal Berthelot, Nicolas Lebegue

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 443 KB

english, 2009

49

Synthesis and in vitro anti-proliferative activity of β-elemene monosubstituted derivatives in HeLa cells mediated through arrest of cell cycle at the G1 phase

Yanhong Sun, Guifeng Liu, Yuangqing Zhang, Hua Zhu, Yunfeng Ren, Yu-Mei Shen

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 585 KB

english, 2009

50

Solution- and solid-phase synthesis and anti-HIV activity of maslinic acid derivatives containing amino acids and peptides

Andres Parra, Francisco Rivas, Pilar E. Lopez, Andres Garcia-Granados, Antonio Martinez, Fernando Albericio, Nieves Marquez, Eduardo Muñoz

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 339 KB

english, 2009

51

Function-oriented synthesis applied to the anti-botulinum natural product toosendanin

Yuya Nakai, William H. Tepp, Tobin J. Dickerson, Eric A. Johnson, Kim D. Janda

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 400 KB

english, 2009

52

In vitro solubility, stability and permeability of novel quercetin–amino acid conjugates

Mi Kyoung Kim, Kwang-su Park, Woon-seok Yeo, Hyunah Choo, Youhoon Chong

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 398 KB

english, 2009

53

Synthesis and biological evaluation of p-carborane bisphenols and their derivatives: Structure–activity relationship for estrogenic activity

Takumi Ogawa, Kiminori Ohta, Toru Iijima, Tomoharu Suzuki, Shigeru Ohta, Yasuyuki Endo

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 567 KB

english, 2009

54

Novel 6-methanesulfonamide-3,4-methylenedioxyphenyl-N-acylhydrazones: Orally effective anti-inflammatory drug candidates

Jorge L.M. Tributino, Carolina D. Duarte, Rodrigo S. Corrêa, Antonio C. Doriguetto, Javier Ellena, Nelilma C. Romeiro, Newton G. Castro, Ana Luisa P. Miranda, Eliezer J. Barreiro, Carlos A.M. Fraga

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 529 KB

english, 2009

55

Tetrahedron Young Investigator Award for Bioorganic and Medicinal Chemistry

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 89 KB

english, 2009

56

Biographical Sketch: Professor Jonathan Ellman

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 102 KB

english, 2009

57

Editorial board

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 51 KB

english, 2009

58

Graphical contents list

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 1.39 MB

english, 2009

59

Instructions to contributors

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 44 KB

english, 2009

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