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Graphical contents list • CONTENTS LIST PDF (1389 K) | |||
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Examining the correlations between GSK-3 inhibitory properties and anti-convulsant efficacy of valproate and valproate-related compounds • SHORT COMMUNICATION Geoff H. Werstuck, Anna J. Kim, Timothy Brenstrum, Stephan A. Ohnmacht, Ella Panna and Alfredo Capretta SummaryPlus | Full Text + Links | PDF (250 K) | |||
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Determination of the enantiomeric purity of the phytoalexins spirobrassinins by 1H NMR using chiral solvation • SHORT COMMUNICATION M.S.C. Pedras, M. Hossain, M.G. Sarwar and S. Montaut SummaryPlus | Full Text + Links | PDF (274 K) | |||
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2- 2-[3-(Pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl pyridine: a highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist • SHORT COMMUNICATION Dehua Huang, Steve F. Poon, Deborah F. Chapman, Janice Chung, Merryl Cramer, Thomas S. Reger, Jeffrey R. Roppe, Lida Tehrani, Nicholas D.P. Cosford and Nicholas D. Smith SummaryPlus | Full Text + Links | PDF (267 K) | |||
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3-[3-Fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)phenyl]-4-methylpyridine: a highly potent and orally bioavailable metabotropic glutamate subtype 5 (mGlu5) receptor antagonist • SHORT COMMUNICATION Steve F. Poon, Brian W. Eastman, Deborah F. Chapman, Janice Chung, Merryl Cramer, Gregory Holtz, Nicholas D.P. Cosford and Nicholas D. Smith SummaryPlus | Full Text + Links | PDF (267 K) | |||
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Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity • SHORT COMMUNICATION Nicholas D. Smith, Steve F. Poon, Dehua Huang, Mitchell Green, Christopher King, Lida Tehrani, Jeffrey R. Roppe, Janice Chung, Deborah P. Chapman, Merryl Cramer and Nicholas D.P. Cosford SummaryPlus | Full Text + Links | PDF (264 K) | |||
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Expedited SAR study of an mGluR5 antagonists: generation of a focused library using a solution-phase Suzuki coupling methodology • SHORT COMMUNICATION Brian Eastman, Chixu Chen, Nicholas D. Smith, Steven Poon, Janice Chung, Grace Reyes-Manalo, Nicholas D.P. Cosford and Benito Munoz SummaryPlus | Full Text + Links | PDF (262 K) | |||
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Parallel synthesis of acylsemicarbazide libraries: preparation of potent cyclin dependent kinase (cdk) inhibitors • SHORT COMMUNICATION David A. Nugiel, Anup Vidwans and Carolyn D. Dzierba SummaryPlus | Full Text + Links | PDF (254 K) | |||
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Parallel methods for the preparation and SAR exploration of N-ethyl-4-[(8-alkyl-8-aza-bicyclo[3.2.1]oct-3-ylidene)-aryl-methyl]-benzamides, powerful mu and delta opioid agonists • SHORT COMMUNICATION Steven J. Coats, Mark J. Schulz, John R. Carson, Ellen E. Codd, Dennis J. Hlasta, Philip M. Pitis, Dennis J. Stone, Jr., Sui-Po Zhang, Ray W. Colburn and Scott L. Dax SummaryPlus | Full Text + Links | PDF (279 K) | |||
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1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-indoles as novel 5-HT6 receptor ligands • SHORT COMMUNICATION Ronald Bernotas, Steven Lenicek, Schuyler Antane, Guo Ming Zhang, Deborah Smith, Joseph Coupet, Boyd Harrison and Lee E. Schechter SummaryPlus | Full Text + Links | PDF (270 K) | |||
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A 13C NMR approach to categorizing potential limitations of α,β-unsaturated carbonyl systems in drug-like molecules • SHORT COMMUNICATION Kevin P. Cusack, Lee D. Arnold, Claude E. Barberis, Haipeng Chen, Anna M. Ericsson, Georgeen S. Gaza-Bulseco, Thomas D. Gordon, Christine M. Grinnell, Andreas Harsch, Maria Pellegrini and Edit Tarcsa SummaryPlus | Full Text + Links | PDF (283 K) | |||
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Azaadamantane benzamide 5-HT4 agonists: gastrointestinal prokinetic SC-54750 • SHORT COMMUNICATION Daniel P. Becker, Daniel L. Flynn, Robert L. Shone and Gary Gullikson SummaryPlus | Full Text + Links | PDF (266 K) | |||
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Synthesis and evaluation of pyridazinylpiperazines as vanilloid receptor 1 antagonists • SHORT COMMUNICATION Laykea Tafesse, Qun Sun, Lori Schmid, Kenneth J. Valenzano, Yakov Rotshteyn, Xin Su and Donald J. Kyle SummaryPlus | Full Text + Links | PDF (308 K) | |||
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Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer’s disease • SHORT COMMUNICATION Christopher J. Helal,Mark A. Sanner, Christopher B. Cooper, Thomas Gant, Mavis Adam, John C. Lucas, Zhijun Kang, Stanley Kupchinsky, Michael K. Ahlijanian, Bonnie Tate et al. SummaryPlus | Full Text + Links | PDF (288 K) | |||
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Synthesis and antitumor activity of 4-hydroxycoumarin derivatives • SHORT COMMUNICATION Jae-Chul Jung, Ji-Ho Lee, Seikwan Oh, Jae-Gon Lee and Oee-Sook Park SummaryPlus | Full Text + Links | PDF (276 K) | |||
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Novel fibrinogen receptor antagonists. RGDF mimetics, derivatives of 4-(isoindoline-5-yl)amino-4-oxobutyric acid • SHORT COMMUNICATION Andrei A. Krysko, Boris M. Chugunov, Olga L. Malovichko, Sergei A. Andronati, Tatyana A. Kabanova, Tamara L. Karaseva and Anna V. Kiriyak SummaryPlus | Full Text + Links | PDF (248 K) | |||
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Racemic and chiral lactams as potent, selective and functionally active CCR4 antagonists • SHORT COMMUNICATION Bradley Newhouse, Shelley Allen, Benjamin Fauber, Aaron S. Anderson, C. Todd Eary, Joshua D. Hansen, Justin Schiro, John J. Gaudino, Ellen Laird, David Chantry et al. SummaryPlus | Full Text + Links | PDF (281 K) | |||
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Isoxazole carboxylic acids as protein tyrosine phosphatase 1B (PTP1B) inhibitors • SHORT COMMUNICATION Hongyu Zhao, Gang Liu, Zhili Xin, Michael D. Serby, Zhonghua Pei, Bruce G. Szczepankiewicz, Philip J. Hajduk, Cele Abad-Zapatero, Charles W. Hutchins, Thomas H. Lubben et al. SummaryPlus | Full Text + Links | PDF (301 K) | |||
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Structurally simplified macrolactone analogues of halichondrin B • SHORT COMMUNICATION Boris M. Seletsky, Yuan Wang, Lynn D. Hawkins, Monica H. Palme, Gregory J. Habgood, Lucian V. DiPietro, Murray J. Towle, Kathleen A. Salvato, Bruce F. Wels, Kimberley K. Aalfs et al. SummaryPlus | Full Text + Links | PDF (301 K) | |||
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Macrocyclic ketone analogues of halichondrin B • SHORT COMMUNICATION Wanjun Zheng, Boris M. Seletsky, Monica H. Palme, Paul J. Lydon, Lori A. Singer, Charles E. Chase, Charles A. Lemelin, Yongchun Shen, Heather Davis, Lynda Tremblay et al. SummaryPlus | Full Text + Links | PDF (303 K) | |||
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An efficient approach to N-acetyl-D-glucosaminuronic acid-based sialylmimetics as potential sialidase inhibitors • SHORT COMMUNICATION Maretta C. Mann, Robin J. Thomson and Mark von Itzstein SummaryPlus | Full Text + Links | PDF (267 K) | |||
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An effective chromatographic separation of chicken red blood cell coproporphyrinogen oxidase and uroporphyrinogen decarboxylase, two enzymes in heme biosynthesis • SHORT COMMUNICATION Marjorie A. Jones, Munish Taneja, Yan Xu, Wen Chung, Christian M. Stob and Timothy D. Lash SummaryPlus | Full Text + Links | PDF (437 K) | |||
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Nitroxyl (HNO) release from new functionalized N-hydroxyurea-derived acyl nitroso-9,10-dimethylanthracene cycloadducts • SHORT COMMUNICATION Bu-Bing Zeng, Jinming Huang, Marcus W. Wright and S. Bruce King SummaryPlus | Full Text + Links | PDF (281 K) | |||
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Aryl urea analogs with broad-spectrum antibacterial activity • SHORT COMMUNICATION Punit P. Seth, Ray Ranken, Dale E. Robinson, Stephen A. Osgood, Lisa M. Risen, Elizabeth L. Rodgers, Michael T. Migawa, Elizabeth A. Jefferson and Eric E. Swayze SummaryPlus | Full Text + Links | PDF (267 K) | |||
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Nocathiacin I analogues: synthesis, in vitro and in vivo biological activity of novel semi-synthetic thiazolyl peptide antibiotics • SHORT COMMUNICATION B. Narasimhulu Naidu, Margaret E. Sorenson, Yunhui Zhang, Oak K. Kim, John D. Matiskella, John A. Wichtowski, Timothy P. Connolly, Wenying Li, Kin S. Lam, Joanne J. Bronson et al. SummaryPlus | Full Text + Links | PDF (276 K) | |||
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Ketopyrrolidines and ketoazetidines as potent dipeptidyl peptidase IV (DPP IV) inhibitors • SHORT COMMUNICATION Dana Ferraris, Yao-Sen Ko, David Calvin, Tiffany Chiou, Susan Lautar, Bert Thomas, Krystyna Wozniak, Camilo Rojas, Vincent Kalish and Sergei Belyakov SummaryPlus | Full Text + Links | PDF (319 K) | |||
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Dimethoxybenzo[i]phenanthridine-12-carboxylic acid derivatives and 6H-dibenzo[c,h][2,6]naphthyridin-5-ones with potent topoisomerase I-targeting activity and cytotoxicity • SHORT COMMUNICATION Alexander L. Ruchelman, Shejin Zhu, Nai Zhou, Angela Liu, Leroy F. Liu and Edmond J. LaVoie SummaryPlus | Full Text + Links | PDF (274 K) | |||
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Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity • SHORT COMMUNICATION Timothy A. Lewis, Michelle A. Young, Mark P. Arrington, Lynn Bayless, Xiong Cai, Philippe Collart, Joseph B. Eckman, James L. Ellis, Doina G. Ene, Lyn Libertine et al. SummaryPlus | Full Text + Links | PDF (261 K) | |||
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Synthesis and HIV-1 integrase inhibitory activity of dimeric and tetrameric analogs of indolicidin • SHORT COMMUNICATION Krzysztof Krajewski, Christophe Marchand, Ya-Qiu Long, Yves Pommier and Peter P. Roller SummaryPlus | Full Text + Links | PDF (291 K) | |||
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Identification of neutral 4-O-alkyl quinolone nonpeptide GnRH receptor antagonists • SHORT COMMUNICATION Robert J. DeVita, Mamta Parikh, Jinlong Jiang, Jason A. Fair, Jonathan R. Young, Thomas F. Walsh, Mark T. Goulet, Jane-L. Lo, Ning Ren, Joel B. Yudkovitz et al. SummaryPlus | Full Text + Links | PDF (287 K) | |||
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Piperazinebenzylamines as potent and selective antagonists of the human melanocortin-4 receptor • SHORT COMMUNICATION Joseph Pontillo, Joseph A. Tran, Beth A. Fleck, Dragan Marinkovic, Melissa Arellano, Fabio C. Tucci, Marion Lanier, Jodie Nelson, Jessica Parker, JohnSaunders et al. SummaryPlus | Full Text + Links | PDF (296 K) | |||
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QSAR modeling of the MAO inhibitory activity of xanthones derivatives • SHORT COMMUNICATION M.B. Núñez, F.P. Maguna, N.B. Okulik and E.A. Castro SummaryPlus | Full Text + Links | PDF (291 K) | |||
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Synthesis of 61-bis(1-adamantylcarbamoyl)-1,2-methano[60]fullerene and its antagonistic effect on haloperidol-induced catalepsy in mice • SHORT COMMUNICATION Manabu Nakazono, Shigeo Hasegawa, Tsuneyuki Yamamoto and Kiyoshi Zaitsu SummaryPlus | Full Text + Links | PDF (253 K) | |||
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Antioxidant activities of a new lignan and a neolignan from Saururus chinensis • SHORT COMMUNICATION Woo Song Lee, Young-Il Baek, Ju-Ryoung Kim, Kyung-Hyun Cho, Dai-Eun Sok and Tae-Sook Jeong SummaryPlus | Full Text + Links | PDF (343 K) | |||
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Quantitative structure–activity relationship analyses of antioxidant and free radical scavenging activities for hydroxybenzalacetones • SHORT COMMUNICATION Chisako Yamagami, Noriko Motohashi, Tatsuhiko Emoto, Akira Hamasaki, Takao Tanahashi, Naotaka Nagakura and Yoshito Takeuchi SummaryPlus | Full Text + Links | PDF (281 K) | |||
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Synthesis and amine transporter affinities of novel phenyltropane derivatives as potential positron emission tomography (PET) imaging agents • SHORT COMMUNICATION Xuemei Peng, Ao Zhang, Nora S. Kula, Ross J. Baldessarini and John L. Neumeyer SummaryPlus | Full Text + Links | PDF (277 K) | |||
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Synthesis of 5′-substituted fluoro-neplanocin A analogues: importance of a hydrogen bonding donor at 5′-position for the inhibitory activity of S-adenosylhomocysteine hydrolase • SHORT COMMUNICATION Hyung Ryong Moon, Hyun Joo Lee, Kyung Ran Kim, Kang Man Lee, Sang Kook Lee, Hea Ok Kim, Moon Woo Chun and Lak Shin Jeong SummaryPlus | Full Text + Links | PDF (282 K) | |||
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Identification and structure–activity relationship studies of 3-methylene-2-norbornanone as potent anti-proliferative agents presumably working through p53 mediated apoptosis • SHORT COMMUNICATION N. Laxma Reddy, Jeanette Hill, Long Ye, Prabhavathi B. Fernandes and David M. Stout SummaryPlus | Full Text + Links | PDF (270 K) | |||
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Synthesis and CYP24 inhibitory activity of 2-substituted-3,4-dihydro-2H-naphthalen-1-one (tetralone) derivatives • SHORT COMMUNICATION Sook Wah Yee and Claire Simons SummaryPlus | Full Text + Links | PDF (257 K) | |||
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Proposal of new modification technique for linear double-stranded DNAs using the polysaccharide schizopyllan • SHORT COMMUNICATION Takahisa Anada, Hideshi Matsunaga, Ryouji Karinaga, Kazuya Koumoto, Masami Mizu, Koji Nakano, Seiji Shinkai and Kazuo Sakurai SummaryPlus | Full Text + Links | PDF (386 K) | |||
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Topological modeling of lipophilicity, diuretic activity, and carbonic inhibition activity of benzene sulfonamides: a molecular connectivity approach • SHORT COMMUNICATION Mona Jaiswal, Padmakar V. Khadikar and Claudiu T. Supuran SummaryPlus | Full Text + Links | PDF (277 K) | |||
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Myxopyronin B analogs as inhibitors of RNA polymerase, synthesis and biological evaluation • SHORT COMMUNICATION Thomas Doundoulakis, Alan X. Xiang, Ricardo Lira, Konstantinos A. Agrios, Stephen E. Webber, Wes Sisson, Robert M. Aust, Amit M. Shah, Richard E. Showalter, James R. Appleman and Klaus B. Simonsen SummaryPlus | Full Text + Links | PDF (330 K) | |||
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Preparation of a tritiated ginkgolide • SHORT COMMUNICATION Kristian Strømgaard, Makiko Suehiro and Koji Nakanishi SummaryPlus | Full Text + Links | PDF (297 K) | |||
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Intact glycation end products containing carboxymethyl-lysine and glyoxal lysine dimer obtained from synthetic collagen model peptide • SHORT COMMUNICATION Hiroaki Yamada, Tomoko Sasaki, Sachiko Niwa, Tohru Oishi, Michio Murata, Toru Kawakami and Saburo Aimoto SummaryPlus | Full Text + Links | PDF (276 K) | |||
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Pyrazolo[1,5-a]pyrimidines as estrogen receptor ligands: defining the orientation of a novel heterocyclic core • SHORT COMMUNICATION Dennis R. Compton, Kathryn E. Carlson and John A. Katzenellenbogen SummaryPlus | Full Text + Links | PDF (317 K) | |||
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Potent inhibitors of the HIV-1 protease incorporating cyclic urea P1–P2 scaffold • SHORT COMMUNICATION Wieslaw M. Kazmierski, Eric Furfine, Yolanda Gray-Nunez, Andrew Spaltenstein and Lois Wright SummaryPlus | Full Text + Links | PDF (267 K) | |||
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Discovery of potent pyrrolidone-based HIV-1 protease inhibitors with enhanced drug-like properties • SHORT COMMUNICATION Wieslaw M. Kazmierski, Webb Andrews, Eric Furfine, Andrew Spaltenstein and Lois Wright SummaryPlus | Full Text + Links | PDF (300 K) | |||
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Azepinone as a conformational constraint in the design of κ-opioid receptor agonists • SHORT COMMUNICATION Paul A. Tuthill, Pamela R. Seida, William Barker, Joel A. Cassel, Serge Belanger, Robert N. DeHaven, Michael Koblish, Susan L. Gottshall, Patrick J. Little, Diane L. DeHaven-Hudkins and Roland E. Dolle SummaryPlus | Full Text + Links | PDF (370 K) | |||
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Synthesis of fluorinated analogues of SJG-136 and their DNA-binding potential • SHORT COMMUNICATION Ahmed Kamal, P.S.M.M. Reddy, D. Rajasekhar Reddy, E. Laxman and Y.L.N. Murthy SummaryPlus | Full Text + Links | PDF (284 K) | |||
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Carbonic anhydrase inhibitors: inhibition of human cytosolic isozyme II and mitochondrial isozyme V with a series of benzene sulfonamide derivatives • SHORT COMMUNICATION Alessio Innocenti, Jochen Antel, Michael Wurl, Andrea Scozzafava and Claudiu T. Supuran SummaryPlus | Full Text + Links | PDF (269 K) | |||
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Synthesis, radiolabeling, and preliminary biological evaluation of [3H]-1-[(S)-N,O-bis-(isoquinolinesulfonyl)-N-methyl-tyrosyl]-4-(o-tolyl)-piperazine, a potent antagonist radioligand for the P2X7 receptor • SHORT COMMUNICATION Romeo Romagnoli, Pier Giovanni Baraldi, Maria Giovanna Pavani, Mojgan Aghazadeh Tabrizi, Allan R. Moorman, Francesco Di Virgilio, Elena Cattabriga, Cecilia Pancaldi, Stefania Gessi and Pier Andrea Borea SummaryPlus | Full Text + Links | PDF (284 K) | |||
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Corrigendum to “Epibatidine structure–activity relationships”: [Bioorg. Med. Chem. Lett. 14 (2004) 1889] • ERRATUM F. Ivy Carroll SummaryPlus | Full Text + Links | PDF (212 K) | |||
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Editorial board • EDITORIAL BOARD PDF (319 K) | |||
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Contributors to this issue • INDEX PDF (190 K) | |||
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Instructions to contributors • PUBLISHER'S NOTE PDF (70 K) | |||
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