Bioorganic and Medicinal Chemistry: Vol 16, Issue 4

Inhibitors of proteases and amide hydrolases that employ an α-ketoheterocycle as a key enabling functionalityPages 1562-1595Bruce E. Maryanoff and Michael J. Costanzo
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ARTICLES
4.
Oxazaborolidine derivatives inducing autoinducer-2 signal transduction in Vibrio harveyiPages 1596-1604R. Aharoni, M. Bronstheyn, A. Jabbour, B. Zaks, M. Srebnik and D. Steinberg
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5.
An expeditious one-pot synthesis of 1,6-dideoxy-N-alkylated nojirimycin derivatives and their inhibitory effects on the secretion of IFN-γ and IL-4Pages 1605-1612Jian Zhou, Yongmin Zhang, Xia Zhou, Jing Zhou, Li-He Zhang, Xin-Shan Ye and Xiao-Lian Zhang
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6.
Design and synthesis of DPP-IV inhibitors lacking the electrophilic nitrile groupPages 1613-1631Takashi Kondo, Takahiro Nekado, Isamu Sugimoto, Kenya Ochi, Shigeyuki Takai, Atsushi Kinoshita, Akira Hatayama, Susumu Yamamoto, Katsuya Kishikawa, Hisao Nakai and Masaaki Toda
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7.
A novel series of parenteral cephalosporins exhibiting potent activities against both Pseudomonas aeruginosa and other Gram-negative pathogens. Part 2: Synthesis and structure–activity relationshipsPages 1632-1647Kenji Yamawaki, Takashi Nomura, Tatsuro Yasukata, Norihiko Tanimoto, Koichi Uotani, Hideaki Miwa, Yoshinori Yamano, Kei Takeda and Yasuhiro Nishitani
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8.
Design and synthesis of a siderophore conjugate as a potent PSMA inhibitor and potential diagnostic agent for prostate cancerPages 1648-1657Pingyu Ding, Paul Helquist and Marvin J. Miller
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9.
New QSAR combined strategy for the design of A1 adenosine receptor agonistsPages 1658-1675Maykel Pérez González, Pedro Besada, Maria José González Moa, Marta Teijeira and Carmen Terán
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10.
Trypanocidal activity of a new pterocarpan and other secondary metabolites of plants from Northeastern Brazil floraPages 1676-1682Nashira Campos Vieira, Laila Salmen Espíndola, Jaime Martins Santana, Maria Leopoldina Veras, Otília Deusdênia Loiola Pessoa, Sávio Moita Pinheiro, Renata Mendonça de Araújo, Mary Anne Sousa Lima and Edilberto Rocha Silveira
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11.
Novel anti-HIV cyclotriazadisulfonamide derivatives as modeled by ligand- and receptor-based approachesPages 1683-1690Júlia R. Pinheiro, Michelle Bitencourt, Elaine F.F. da Cunha, Teodorico C. Ramalho and Matheus P. Freitas
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12.
Antiproliferative effects on human tumor cells and rat aortic smooth muscular cells of 2,3-heteroarylmaleimides and heterofused imidesPages 1691-1701Nicola Ferri, Egle Maria Beccalli, Alessandro Contini, Alberto Corsini, Manuela Antonino, Tiziano Radice, Graziella Pratesi, Stella Tinelli, Franco Zunino and Maria Luisa Gelmi
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13.
Conception of myeloperoxidase inhibitors derived from flufenamic acid by computational docking and structure modificationPages 1702-1720Pierre Van Antwerpen, Martine Prévost, Karim Zouaoui-Boudjeltia, Sajida Babar, I. Legssyer, Patrick Moreau, Nicole Moguilevsky, Michel Vanhaeverbeek, Jean Ducobu, Jean Nève and François Dufrasne
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14.
Synthesis, characterization and antiproliferative studies of the enantiomers of cis-[(1,2-camphordiamine)dichloro]platinum(II) complexesPages 1721-1737Ángel M. Montaña, Francisco J. Bernal, Julia Lorenzo, Carlos Farnós, Consuelo Batalla, Maria J. Prieto, Virtudes Moreno, Francesc X. Avilés, Juan M. Mesas and María-Teresa Alegre
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15.
Iromycins from Streptomyces sp. and from synthesis: New inhibitors of the mitochondrial electron transport chainPages 1738-1746Frank Surup, Heydar Shojaei, Paultheo von Zezschwitz, Brigitte Kunze and Stephanie Grond
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16.
Protein phosphatase inhibitory activity of tautomycin photoaffinity probes evaluated at femto-molar levelPages 1747-1755Magne O. Sydnes, Masaki Kuse, Masakuni Kurono, Aya Shimomura, Hiroshi Ohinata, Akira Takai and Minoru Isobe
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17.
A novel sesquiterpenoid dimer parviflorene F induces apoptosis by up-regulating the expression of TRAIL-R2 and a caspase-dependent mechanismPages 1756-1763Takashi Ohtsuki, Mayu Tamaki, Kazuhumi Toume and Masami Ishibashi
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18.
Toward the development of chemoprevention agents (III): Synthesis and anti-inflammatory activities of a new class of 5-glycylamino-2-substituted-phenyl-1,3-dioxacycloalkanesPages 1764-1774Lanrong Bi, Ming Zhao, Keli Gu, Chao Wang, Jingfang Ju and Shiqi Peng
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19.
Synthesis, metal ion binding, and biological evaluation of new anticancer 2-(2′-hydroxyphenyl)benzoxazole analogs of UK-1Pages 1775-1783Mireya L. McKee and Sean M. Kerwin
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20.
Virtual screening approaches for the identification of non-lipid autotaxin inhibitorsPages 1784-1795Abby L. Parrill, Uniqua Echols, Tran Nguyen, Truc-Chi T. Pham, Adrienne Hoeglund and Daniel L. Baker
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21.
Synthesis and structure–activity relationships of 16-ene-22-thia-1α,25-dihydroxy-26,27-dimethyl-19-norvitamin D3 analogs having side chains of different sizesPages 1796-1815Hajime Takaku, Yukiko Miyamoto, Shiori Asami, Mika Shimazaki, Sachiko Yamada, Keiko Yamamoto, Nobuyuki Udagawa, Hector F. DeLuca and Masato Shimizu
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22.
Orally active 1,2,4-trioxepanes: Synthesis and antimalarial activity of a series of 7-arylvinyl-1,2,4-trioxepanes against multidrug-resistant Plasmodium yoelii in Swiss micePages 1816-1821Chandan Singh, Shilpi Pandey, Malvika Sharma and Sunil K. Puri
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23.
Design, Synthesis and Evaluation of Antiinflammatory, Analgesic and Ulcerogenicity studies of Novel S-Substituted phenacyl-1,3,4-oxadiazole-2-thiol and Schiff bases of Diclofenac acid as Nonulcerogenic DerivativesPages 1822-1831Shashikant V. Bhandari, Kailash G. Bothara, Mayuresh K. Raut, Ajit A. Patil, Aniket P. Sarkate and Vinod J. Mokale
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24.
The synthesis of bivalent 2β-carbomethoxy-3β-(3,4-dichlorophenyl)-8-heterobicyclo[3.2.1]octanes as probes for proximal binding sites on the dopamine and serotonin transportersPages 1832-1841Peter C. Meltzer, Olga Kryatova, Duy-Phong Pham-Huu, Patrick Donovan and Aaron Janowsky
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25.
Influence of heterocyclic and oxime-containing farnesol analogs on quorum sensing and pathogenicity in Candida albicansPages 1842-1848Roman Shchepin, Dhammika H.M.L.P. Navarathna, Raluca Dumitru, Shane Lippold, Kenneth W. Nickerson and Patrick H. Dussault
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26.
Estradiol and estrone C-16 derivatives as inhibitors of type 1 17β-hydroxysteroid dehydrogenase: Blocking of ER+ breast cancer cell proliferation induced by estronePages 1849-1860Yannick Laplante, Christine Cadot, Michelle-Audrey Fournier and Donald Poirier
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27.
N6-substituted C5′-modified adenosines as A1 adenosine receptor agonistsPages 1861-1873T.D. Ashton, Stephen P. Baker, Sally A. Hutchinson and Peter J. Scammells
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28.
Potent and selective small molecule NS3 serine protease inhibitors of Hepatitis C virus with dichlorocyclopropylproline as P2 residuePages 1874-1883Kevin X. Chen, Bancha Vibulbhan, Weiying Yang, Kuo-Chi Cheng, Rong Liu, John Pichardo, Nancy Butkiewicz and F. George Njoroge
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29.
Biomimetic synthesis of xuxuarines Eα and Eβ: Structure revision of Rzedowskia bistriterpenoidsPages 1884-1889Neil E. Jacobsen, E.M. Kithsiri Wijeratne, Joaquim Corsino, Maysa Furlan, Vanderlan da S. Bolzani and A.A. Leslie Gunatilaka
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30.
5,5,6-Fused tricycles bearing imidazole and pyrazole 6-methylidene penems as broad-spectrum inhibitors of β-lactamasesPages 1890-1902Aranapakam M. Venkatesan, Atul Agarwal, Takao Abe, Hideki Ushirogochi, Mihira Ado, Takasaki Tsuyoshi, Osvaldo Dos Santos, Zhong Li, Gerry Francisco, Yang I. Lin, Peter J. Petersen, Youjun Yang, William J. Weiss, David M. Shlaes and Tarek S. Mansour
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31.
Selection and characterization of human antibodies neutralizing Bacillus anthracis toxinPages 1903-1913Bin Zhou, Charlotte Carney and Kim D. Janda
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32.
A comparative molecular field and comparative molecular similarity indices analyses (CoMFA and CoMSIA) of N-phenyl-N′-(2-chloroethyl)ureas targeting the colchicine-binding site as anticancer agentsPages 1914-1926Sébastien Fortin, Philippe Labrie, Emmanuel Moreau, Lianhu Wei, Lakshmi P. Kotra and René C.-Gaudreault
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33.
Anti-Plasmodium activity of tetrazolium saltsPages 1927-1947Xilin Cui, Jason Z. Vlahakis, Ian E. Crandall and Walter A. Szarek
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34.
Synthesis and cyclooxygenase inhibitory activities of linear 1-(methanesulfonylphenyl or benzenesulfonamido)-2-(pyridyl)acetylene regioisomersPages 1948-1956Morshed Alam Chowdhury, Ying Dong, Qiao-Hong Chen, Khaled R.A. Abdellatif and Edward E. Knaus
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35.
New 1,2,3,4-tetrahydroisoquinoline derivatives as modulators of proteolytic cleavage of amyloid precursor proteinsPages 1957-1965Ming-Kuan Hu, Yung-Feng Liao, Jung-Fang Chen, Bo-Jeng Wang, Ying-Tsen Tung, Hui-Ching Lin and Kang-Po Lee
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36.
Synthesis and structure–activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonistsPages 1966-1982Itsuro Shimada, Kyoichi Maeno, Ken-ichi Kazuta, Hideki Kubota, Tetsuya Kimizuka, Yasuharu Kimura, Ken-ichi Hatanaka, Yuki Naitou, Fumikazu Wanibuchi, Shuichi Sakamoto and Shin-ichi Tsukamoto
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37.
Properties of flaky affinity resin with co-continuous structurePages 1983-1991Tomoko Mori, Akito Tanaka, Takuya Kubo, Kunimitsu Kaya, Mari Sakamoto and Ken Hosoya
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38.
Synthesis, biological evaluation and molecular modelling studies of methyleneimidazole substituted biaryls as inhibitors of human 17α-hydroxylase-17,20-lyase (CYP17). Part I: Heterocyclic modifications of the core structurePages 1992-2010Carsten Jagusch, Matthias Negri, Ulrike E. Hille, Qingzhong Hu, Marc Bartels, Kerstin Jahn-Hoffmann, Mariano A.E. Pinto-Bazurco Mendieta, Barbara Rodenwaldt, Ursula Müller-Vieira, Dirk Schmidt, Thomas Lauterbach, Maurizio Recanatini, Andrea Cavalli and Rolf W. Hartmann
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39.
Phenylalanine-containing hydroxamic acids as selective inhibitors of class IIb histone deacetylases (HDACs)Pages 2011-2033Stefan Schäfer, Laura Saunders, Elena Eliseeva, Alfredo Velena, Mira Jung, Andreas Schwienhorst, Anja Strasser, Achim Dickmanns, Ralf Ficner, Sonja Schlimme, Wolfgang Sippl, Eric Verdin and Manfred Jung
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40.
The effect of flavonoid derivatives on doxorubicin transport and metabolismPages 2034-2042Radka Václavíková, Eliška Kondrová, Marie Ehrlichová, Ahcene Boumendjel, Jan Kovář, Pavel Stopka, Pavel Souček and Ivan Gut
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41.
Aryl azoles with neuroprotective activity—Parallel synthesis and attempts at target identificationPages 2043-2052Giuseppe Cocconcelli, Enrica Diodato, Andrea Caricasole, Giovanni Gaviraghi, Eva Genesio, Chiara Ghiron, Letizia Magnoni, Elena Pecchioli, Pier Vincenzo Plazzi and Georg C. Terstappen
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42.
Design of azidoproline containing gluten peptides to suppress CD4+ T-cell responses associated with Celiac diseasePages 2053-2062Varsha V. Kapoerchan, Martina Wiesner, Mark Overhand, Gijs A. van der Marel, Frits Koning and Herman S. Overkleeft
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43.
Synthesis of novel spirostanic saponins and their cytotoxic activityPages 2063-2076Juan C. Hernández, Francisco León, Ignacio Brouard, Fernando Torres, Sara Rubio, José Quintana, Francisco Estévez and Jaime Bermejo
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44.
Corrugoside, a new immunostimulatory α-galactoglycosphingolipid from the marine sponge Axinella corrugataPages 2077-2085Valeria Costantino, Ernesto Fattorusso, Concetta Imperatore, Alfonso Mangoni, Stefan Freigang and Luc Teyton
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45.
Synthesis of (nor)tropeine (di)esters and allosteric modulation of glycine receptor bindingPages 2086-2092Gábor Maksay, Péter Nemes, Zoltán Vincze and Timea Bíró
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46.
Targeting the inverted CCAAT Box-2 of the topoisomerase IIα gene: DNA sequence selective recognition by a polyamide–intercalator as a staggered dimerPages 2093-2102Hilary Mackay, Toni Brown, Jim S. Sexton, Minal Kotecha, Binh Nguyen, W. David Wilson, Jerome Kluza, Boris Savic, Caroline O’Hare, Daniel Hochhauser, Moses Lee and John A. Hartley
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47.
Synthesis, adenosine receptor binding and 3D-QSAR of 4-substituted 2-(2′-furyl)-1,2,4-triazolo[1,5-a]quinoxalinesPages 2103-2113Ana Martínez, Hugo Gutiérrez-de-Terán, José Brea, Enrique Raviña, Maria Isabel Loza, Maria Isabel Cadavid, Ferran Sanz, Bernat Vidal, Victor Segarra and Eddy Sotelo
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48.
Influence of sulfur oxidation state and steric bulk upon trifluoromethyl ketone (TFK) binding kinetics to carboxylesterases and fatty acid amide hydrolase (FAAH)Pages 2114-2130Craig E. Wheelock, Kosuke Nishi, Andy Ying, Paul D. Jones, Michael E. Colvin, Marilyn M. Olmstead and Bruce D. Hammock
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49.
Bioorganic & Medicinal Chemistry Reviews and PerspectivesPages 2131-2133
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50.
Instructions to contributorsPage I
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