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Medicinal Chemistry: Current Research Articles


 
Current research articles in the field of Medicinal Chemistry published in online journals.

The author- or copyrights of the listed research articles below are held by the respective authors or site operators, who are also responsible for the content of the presentations.

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On this page considered biochemistry journals:


Journal of Medicinal Chemistry - published by The American Chemical Society, ACS -
As the most cited journal in Medicinal Chemistry, the Journal of Medicinal Chemistry focuses on original research dealing with chemical-biological relationships, mainly the bond between molecular structure and biological activity.

Enzyme Inhibition and Medicinal Chem - published by Taylor & Francis -
... is an international and interdisciplinary vehicle publishing new knowledge and findings on enzyme inhibitors and inhibitory processes and agonist/antagonist receptor interactions in the development of medicinal and anti-cancer agents and an understanding of their action.

Medicinal Chemistry Research - published by Springer -
... offers prompt publication of novel experimental achievements in the many facets of drug design, drug discovery, and the elucidation of mechanisms of action of biologically active compounds.



Current research articles of the mentioned journals:


Discovery of 2-Chloro-N-(4-methoxyphenyl)-N-methylquinazolin-4-amine (EP128265, MPI-0441138) as a Potent Inducer of Apoptosis with High In Vivo Activity

Nilantha Sirisoma, Shailaja Kasibhatla, Azra Pervin, Hong Zhang, Songchun Jiang, J. Adam Willardsen, Mark B. Anderson, Vijay Baichwal, Gary G. Mather, Kevin Jessing, Raouf Hussain, Khanh Hoang, Christopher M. Pleiman, Ben Tseng, John Drewe, and Sui Xiong Cai
Web Release Date: Thu, 24 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm8003653

Source: Journal of Medicinal Chemistry | 24 Jul 2008 | 6:00 am CEST

Journal of Medicinal Chemistry

Journal of Medicinal Chemistry, Volume 51 Issue 14 (July 24, 2008) is now available

Source: Journal of Medicinal Chemistry | 24 Jul 2008 | 6:00 am CEST

Synthesis of GABAA Receptor Agonists and Evaluation of their α-Subunit Selectivity and Orientation in the GABA Binding Site

Michaela Jansen, Holger Rabe, Axelle Strehless, Sandra Dieler, Fabian Debus, Gerd Dannhardt, Myles H. Akabas, and Hartmut Lüddens
Web Release Date: Thu, 24 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm701562x

Source: Journal of Medicinal Chemistry | 24 Jul 2008 | 6:00 am CEST

Design, Synthesis and Biological Evaluation of Glutathione Peptidomimetics as Components of Anti-Parkinson Prodrugs

Swati S. More and Robert Vince
Web Release Date: Thu, 24 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800239v

Source: Journal of Medicinal Chemistry | 24 Jul 2008 | 6:00 am CEST

Discovery of a Novel Series of Benzoic Acid Derivatives as Potent and Selective Human β3 Adrenergic Receptor Agonists with Good Oral Bioavailability. 3. Phenylethanolaminotetraline (PEAT) Skeleton Containing Biphenyl or Biphenyl Ether Moiety

Masashi Imanishi, Yutaka Nakajima, Yasuyo Tomishima, Hitoshi Hamashima, Kenichi Washizuka, Minoru Sakurai, Shigeo Matsui, Emiko Imamura, Koji Ueshima, Takao Yamamoto, Nobuhiro Yamamoto, Hirofumi Ishikawa, Keiko Nakano, Naoko Unami, Kaori Hamada, Yasuhiro Matsumura, Fujiko Takamura, and Kouji Hattori
Web Release Date: Thu, 24 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800222k

Source: Journal of Medicinal Chemistry | 24 Jul 2008 | 6:00 am CEST

Design of a Sialylglycopolymer with a Chitosan Backbone Having Efficient Inhibitory Activity against Influenza Virus Infection

Myco Umemura, Masae Itoh, Yutaka Makimura, Kohji Yamazaki, Midori Umekawa, Ayano Masui, Yoshiharu Matahira, Mari Shibata, Hisashi Ashida, and Kenji Yamamoto
Web Release Date: Thu, 24 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm8000967

Source: Journal of Medicinal Chemistry | 24 Jul 2008 | 6:00 am CEST

Identification of 4-Aminopyrazolylpyrimidines as Potent Inhibitors of Trk Kinases

Tao Wang, Michelle L. Lamb, David A. Scott, Haixia Wang, Michael H. Block, Paul D. Lyne, John W. Lee, Audrey M. Davies, Hai-Jun Zhang, Yanyi Zhu, Fei Gu, Yongxin Han, Bin Wang, Peter J. Mohr, Robert J. Kaus, John A. Josey, Ethan Hoffmann, Ken Thress, Terry MacIntyre, Haiyun Wang, Charles A. Omer, and Dingwei Yu
Web Release Date: Wed, 23 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800343j

Source: Journal of Medicinal Chemistry | 23 Jul 2008 | 6:00 am CEST

False Positives in a Reporter Gene Assay: Identification and Synthesis of Substituted N-Pyridin-2-ylbenzamides as Competitive Inhibitors of Firefly Luciferase

Laura H. Heitman, Jacobus P. D. van Veldhoven, Annelien M. Zweemer, Kai Ye, Johannes Brussee, and Adriaan P. IJzerman
Web Release Date: Wed, 23 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm8004509

Source: Journal of Medicinal Chemistry | 23 Jul 2008 | 6:00 am CEST

Novel Quinolinonyl Diketo Acid Derivatives as HIV-1 Integrase Inhibitors: Design, Synthesis, and Biological Activities

Roberto Di Santo, Roberta Costi, Alessandra Roux, Gaetano Miele, Giuliana Cuzzucoli Crucitti, Alberto Iacovo, Federica Rosi, Antonio Lavecchia, Luciana Marinelli, Carmen Di Giovanni, Ettore Novellino, Lucia Palmisano, Mauro Andreotti, Roberta Amici, Clementina Maria Galluzzo, Lucia Nencioni, Anna Teresa Palamara, Yves Pommier, and Christophe Marchand
Web Release Date: Wed, 23 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm8001422

Source: Journal of Medicinal Chemistry | 23 Jul 2008 | 6:00 am CEST

Oxadiazole-carbonylaminothioureas as SIRT1 and SIRT2 Inhibitors

Tero Huhtiniemi, Tiina Suuronen, Valtteri M. Rinne, Carsten Wittekindt, Maija Lahtela-Kakkonen, Elina Jarho, Erik A. A. Wallén, Antero Salminen, Antti Poso, and Jukka Leppänen
Web Release Date: Tue, 22 Jul 2008 00:00:00 EDT (Letter) DOI: 10.1021/jm800639h

Source: Journal of Medicinal Chemistry | 22 Jul 2008 | 6:00 am CEST

Use of the Nitrile Oxide Cycloaddition (NOC) Reaction for Molecular Probe Generation: A New Class of Enzyme Selective Histone Deacetylase Inhibitors (HDACIs) Showing Picomolar Activity at HDAC6

Alan P. Kozikowski, Subhasish Tapadar, Doris N. Luchini, Ki Hwan Kim, and Daniel D. Billadeau
Web Release Date: Tue, 22 Jul 2008 00:00:00 EDT (Letter) DOI: 10.1021/jm8002894

Source: Journal of Medicinal Chemistry | 22 Jul 2008 | 6:00 am CEST

Novel Analogues of Istaroxime, a Potent Inhibitor of Na+,K+-ATPase: Synthesis and Structure−Activity Relationship

Mauro Gobbini, Silvia Armaroli, Leonardo Banfi, Alessandra Benicchio, Giulio Carzana, Giorgio Fedrizzi, Patrizia Ferrari, Giuseppe Giacalone, Michele Giubileo, Giuseppe Marazzi, Rosella Micheletti, Barbara Moro, Marco Pozzi, Piero Enrico Scotti, Marco Torri, and Alberto Cerri
Web Release Date: Sat, 19 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800257s

Source: Journal of Medicinal Chemistry | 19 Jul 2008 | 6:00 am CEST

Novel 4-Aminoquinolines Active against Chloroquine-Resistant and Sensitive P. falciparum Strains that also Inhibit Botulinum Serotype A

Bogdan A. Šolaja, Dejan Opsenica, Kirsten S. Smith, Wilbur K. Milhous, Nataša Terzić, Igor Opsenica, James C. Burnett, Jon Nuss, Rick Gussio, and Sina Bavari
Web Release Date: Sat, 19 Jul 2008 00:00:00 EDT (Letter) DOI: 10.1021/jm800737y

Source: Journal of Medicinal Chemistry | 19 Jul 2008 | 6:00 am CEST

Synthesis and Evaluation of Technetium-99m- and Rhenium-Labeled Inhibitors of the Prostate-Specific Membrane Antigen (PSMA)

Sangeeta R. Banerjee, Catherine A. Foss, Mark Castanares, Ronnie C. Mease, Youngjoo Byun, James J. Fox, John Hilton, Shawn E. Lupold, Alan P. Kozikowski, and Martin G. Pomper
Web Release Date: Sat, 19 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800111u

Source: Journal of Medicinal Chemistry | 19 Jul 2008 | 6:00 am CEST

(9S)-9-(2-Hydroxy-4,4-dimethyl-6-oxo-1-cyclohexen-1-yl)-3,3-dimethyl-2,3,4,9-tetrahydro-1H-xanthen-1-one, a Selective and Orally Active Neuropeptide Y Y5 Receptor Antagonist

Nagaaki Sato, Makoto Jitsuoka, Takunobu Shibata, Tomoko Hirohashi, Katsumasa Nonoshita, Minoru Moriya, Yuji Haga, Aya Sakuraba, Makoto Ando, Tomoyuki Ohe, Hisashi Iwaasa, Akira Gomori, Akane Ishihara, Akio Kanatani, and Takehiro Fukami
Web Release Date: Sat, 19 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm8003587

Source: Journal of Medicinal Chemistry | 19 Jul 2008 | 6:00 am CEST

2-Amino-6-furan-2-yl-4-substituted Nicotinonitriles as A2A Adenosine Receptor Antagonists

Monica Mantri, Olivier de Graaf, Jacobus van Veldhoven, Anikó Göblyös, Jacobien K. von Frijtag Drabbe Künzel, Thea Mulder-Krieger, Regina Link, Henk de Vries, Margot W. Beukers, Johannes Brussee, and Adriaan P. IJzerman
Web Release Date: Sat, 19 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm701594y

Source: Journal of Medicinal Chemistry | 19 Jul 2008 | 6:00 am CEST

Ethyl 8-Fluoro-6-(3-nitrophenyl)-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate as Novel, Highly Potent, and Safe Antianxiety Agent

Maurizio Anzini, Carlo Braile, Salvatore Valenti, Andrea Cappelli, Salvatore Vomero, Luciana Marinelli, Vittorio Limongelli, Ettore Novellino, Laura Betti, Gino Giannaccini, Antonio Lucacchini, Carla Ghelardini, Monica Norcini, Francesco Makovec, Gianluca Giorgi, and R. Ian Fryer
Web Release Date: Sat, 19 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm8002944

Source: Journal of Medicinal Chemistry | 19 Jul 2008 | 6:00 am CEST

Structure−Antitussive Activity Relationships of Naltrindole Derivatives. Identification of Novel and Potent Antitussive Agents

Satoshi Sakami, Masayuki Maeda, Koji Kawai, Takumi Aoki, Kuniaki Kawamura, Hideaki Fujii, Ko Hasebe, Mayumi Nakajima, Takashi Endo, Shinya Ueno, Tsuyoshi Ito, Junzo Kamei, and Hiroshi Nagase
Web Release Date: Sat, 19 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm701440h

Source: Journal of Medicinal Chemistry | 19 Jul 2008 | 6:00 am CEST

A Pentacyclic Aurora Kinase Inhibitor (AKI-001) with High in Vivo Potency and Oral Bioavailability

Thomas E. Rawson, Matthias Rüth, Elizabeth Blackwood, Dan Burdick, Laura Corson, Jenna Dotson, Jason Drummond, Carter Fields, Guy J. Georges, Bernhard Goller, Jason Halladay, Thomas Hunsaker, Tracy Kleinheinz, Hans-Willi Krell, Jun Li, Jun Liang, Anja Limberg, Angela McNutt, John Moffat, Gail Phillips, Yingqing Ran, Brian Safina, Mark Ultsch, Leslie Walker, Christian Wiesmann, Birong Zhang, Aihe Zhou, Bing-Yan Zhu, Petra Rüger, and Andrea G. Cochran
Web Release Date: Thu, 17 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800052b

Source: Journal of Medicinal Chemistry | 17 Jul 2008 | 6:00 am CEST

Structure-Based Development of Novel Adenylyl Cyclase Inhibitors

Christine Schlicker, Annika Rauch, Ken C. Hess, Barbara Kachholz, Lonny R. Levin, Jochen Buck, and Clemens Steegborn
Web Release Date: Thu, 17 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800481q

Source: Journal of Medicinal Chemistry | 17 Jul 2008 | 6:00 am CEST

Substituted 6-Phenyl-2-naphthols. Potent and Selective Nonsteroidal Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1): Design, Synthesis, Biological Evaluation, and Pharmacokinetics

Sandrine Marchais-Oberwinkler, Patricia Kruchten, Martin Frotscher, Erika Ziegler, Alexander Neugebauer, Umadevi Bhoga, Emmanuel Bey, Ursula Müller-Vieira, Josef Messinger, Hubert Thole, and Rolf W. Hartmann
Web Release Date: Thu, 17 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800367k

Source: Journal of Medicinal Chemistry | 17 Jul 2008 | 6:00 am CEST

Identification and Validation of Human DNA Ligase Inhibitors Using Computer-Aided Drug Design

Shijun Zhong, Xi Chen, Xiao Zhu, Barbara Dziegielewska, Kurtis E. Bachman, Tom Ellenberger, Jeff D. Ballin, Gerald M. Wilson, Alan E. Tomkinson, and Alexander D. MacKerell Jr.
Web Release Date: Thu, 17 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm8001668

Source: Journal of Medicinal Chemistry | 17 Jul 2008 | 6:00 am CEST

Design, Synthesis, and Biological Evaluation of 14-Substituted Aromathecins as Topoisomerase I Inhibitors

Maris A. Cinelli, Andrew Morrell, Thomas S. Dexheimer, Evan S. Scher, Yves Pommier, and Mark Cushman
Web Release Date: Thu, 17 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800259e

Source: Journal of Medicinal Chemistry | 17 Jul 2008 | 6:00 am CEST

5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a Series of Anti-HIV-1 Agents of the Dihydro-alkoxy-benzyl-oxopyrimidine Family with Peculiar Structure−Activity Relationship Profile

Maxim B. Nawrozkij, Dante Rotili, Domenico Tarantino, Giorgia Botta, Alexandre S. Eremiychuk, Ira Musmuca, Rino Ragno, Alberta Samuele, Samantha Zanoli, Mercedes Armand-Ugón, Imma Clotet-Codina, Ivan A. Novakov, Boris S. Orlinson, Giovanni Maga, José A. Esté, Marino Artico, and Antonello Mai
Web Release Date: Thu, 17 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800340w

Source: Journal of Medicinal Chemistry | 17 Jul 2008 | 6:00 am CEST

Slow Self-Activation Enhances The Potency of Viridin Prodrugs

Joseph Blois, Hushan Yuan, Adam Smith, Michael E. Pacold, Ralph Weissleder, Lewis C. Cantley, and Lee Josephson
Web Release Date: Thu, 17 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800374f

Source: Journal of Medicinal Chemistry | 17 Jul 2008 | 6:00 am CEST

Book Review of Biosimulation in Drug Development

Kevin D. Hall
Web Release Date: Thu, 17 Jul 2008 00:00:00 EDT (Book Review) DOI: 10.1021/jm800678c

Source: Journal of Medicinal Chemistry | 17 Jul 2008 | 6:00 am CEST

Selective Nucleoside Triphosphate Diphosphohydrolase-2 (NTPDase2) Inhibitors: Nucleotide Mimetics Derived from Uridine-5′-carboxamide

Andreas Brunschweiger, Jamshed Iqbal, Frank Umbach, Anja B. Scheiff, Mercedes N. Munkonda, Jean Sévigny, Aileen F. Knowles, and Christa E Müller
Web Release Date: Thu, 17 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800175e

Source: Journal of Medicinal Chemistry | 17 Jul 2008 | 6:00 am CEST

Book Review of Drug Metabolism. Chemical and Enzymatic Aspects

Manfred E. Wolff
Web Release Date: Thu, 17 Jul 2008 00:00:00 EDT (Book Review) DOI: 10.1021/jm800706c

Source: Journal of Medicinal Chemistry | 17 Jul 2008 | 6:00 am CEST

Optimization of the Central Heterocycle of α-Ketoheterocycle Inhibitors of Fatty Acid Amide Hydrolase

Joie Garfunkle, Cyrine Ezzili, Thomas J. Rayl, Dustin G. Hochstatter, Inkyu Hwang, and Dale L. Boger
Web Release Date: Wed, 16 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800136b

Source: Journal of Medicinal Chemistry | 16 Jul 2008 | 6:00 am CEST

Influence of Conformational Flexibility on Complexation-Induced Changes in Chemical Shift in a Neocarzinostatin Protein−Ligand Complex

Marina Cioffi, Christopher A. Hunter, and Martin J. Packer
Web Release Date: Tue, 15 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800075r

Source: Journal of Medicinal Chemistry | 15 Jul 2008 | 6:00 am CEST

High Affinity Conformationally Constrained Nociceptin/Orphanin FQ(1−13) Amide Analogues

Laksana Charoenchai, Hongyan Wang, Jia Bei Wang, and Jane V. Aldrich
Web Release Date: Tue, 15 Jul 2008 00:00:00 EDT (Letter) DOI: 10.1021/jm800394v

Source: Journal of Medicinal Chemistry | 15 Jul 2008 | 6:00 am CEST

Targeting the Lysosome: Fluorescent Iron(III) Chelators To Selectively Monitor Endosomal/Lysosomal Labile Iron Pools

Sarah Fakih, Maria Podinovskaia, Xiaole Kong, Helen L. Collins, Ulrich E. Schaible, and Robert C. Hider
Web Release Date: Tue, 15 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm8001247

Source: Journal of Medicinal Chemistry | 15 Jul 2008 | 6:00 am CEST

Novel Terphenyls and 3,5-Diaryl Isoxazole Derivatives Endowed with Growth Supporting and Antiapoptotic Properties

Daniele Simoni, Riccardo Rondanin, Riccardo Baruchello, Michele Rizzi, Giuseppina Grisolia, Marco Eleopra, Stefania Grimaudo, Antonietta Di Cristina, Maria Rosaria Pipitone, Maria Rita Bongiorno, Mario Aricò, Francesco Paolo Invidiata, and Manlio Tolomeo
Web Release Date: Sat, 12 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800388m

Source: Journal of Medicinal Chemistry | 12 Jul 2008 | 6:00 am CEST

Discovery of 5-[[4-[(2,3-Dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a Novel and Potent Vascular Endothelial Growth Factor Receptor Inhibitor

Philip A. Harris, Amogh Boloor, Mui Cheung, Rakesh Kumar, Renae M. Crosby, Ronda G. Davis-Ward, Andrea H. Epperly, Kevin W. Hinkle, Robert N. Hunter III, Jennifer H. Johnson, Victoria B. Knick, Christopher P. Laudeman, Deirdre K. Luttrell, Robert A. Mook, Robert T. Nolte, Sharon K. Rudolph, Jerzy R. Szewczyk, Anne T. Truesdale, James M. Veal, Liping Wang, and Jeffrey A. Stafford
Web Release Date: Sat, 12 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800566m

Source: Journal of Medicinal Chemistry | 12 Jul 2008 | 6:00 am CEST

Novel Indoline-Based Acyl-CoA:Cholesterol Acyltransferase Inhibitor with Antiperoxidative Activity: Improvement of Physicochemical Properties and Biological Activities by Introduction of Carboxylic Acid

Kenji Takahashi, Masayasu Kasai, Masaru Ohta, Yoshimichi Shoji, Kazuyoshi Kunishiro, Mamoru Kanda, Kazuyoshi Kurahashi, and Hiroaki Shirahase
Web Release Date: Sat, 12 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800248r

Source: Journal of Medicinal Chemistry | 12 Jul 2008 | 6:00 am CEST

Selectivity Determinants of Inhibitor Binding to Human 20α-Hydroxysteroid Dehydrogenase: Crystal Structure of the Enzyme in Ternary Complex with Coenzyme and the Potent Inhibitor 3,5-Dichlorosalicylic Acid

Urmi Dhagat, Satoshi Endo, Rie Sumii, Akira Hara, and Ossama El-Kabbani
Web Release Date: Sat, 12 Jul 2008 00:00:00 EDT (Brief Article) DOI: 10.1021/jm8003575

Source: Journal of Medicinal Chemistry | 12 Jul 2008 | 6:00 am CEST

Chemical Proteomics-Based Drug Design: Target and Antitarget Fishing with a Catechol−Rhodanine Privileged Scaffold for NAD(P)(H) Binding Proteins

Xia Ge, Bassam Wakim, and Daniel S. Sem
Web Release Date: Fri, 11 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm8002284

Source: Journal of Medicinal Chemistry | 11 Jul 2008 | 6:00 am CEST

Methyl (11aS)-1,2,3,5,11,11a-Hexahydro-3,3-dimethyl-1-oxo-6H-imidazo-[3′,4′:1,2]pyridin[3,4-b]indol-2-Substituted Acetates: Synthesis and Three-Dimensional Quantitative Structure−Activity Relationship Investigation as a Class of Novel Vasodilators

Jiawang Liu, Ming Zhao, Guohui Cui, Xiaoyi Zhang, Jun Wang, and Shiqi Peng
Web Release Date: Fri, 11 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800249j

Source: Journal of Medicinal Chemistry | 11 Jul 2008 | 6:00 am CEST

Structure of Daidzin, a Naturally Occurring Anti-Alcohol-Addiction Agent, in Complex with Human Mitochondrial Aldehyde Dehydrogenase

Edward D. Lowe, Guang-Yao Gao, Louise N. Johnson, and Wing Ming Keung
Web Release Date: Thu, 10 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800488j

Source: Journal of Medicinal Chemistry | 10 Jul 2008 | 6:00 am CEST

Naturally Occurring Homoisoflavonoids Function as Potent Protein Tyrosine Kinase Inhibitors by c-Src-Based High-Throughput Screening

Li-Gen Lin, Hua Xie, Hong-Lin Li, Lin-Jiang Tong, Chun-Ping Tang, Chang-Qiang Ke, Qun-Fang Liu, Li-Ping Lin, Mei-Yu Geng, Hualiang Jiang, Wei-Min Zhao, Jian Ding, and Yang Ye
Web Release Date: Wed, 9 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm701501x

Source: Journal of Medicinal Chemistry | 9 Jul 2008 | 6:00 am CEST

The Structural Basis for Peptidomimetic Inhibition of Eukaryotic Ribonucleotide Reductase: A Conformationally Flexible Pharmacophore

Hai Xu, James W. Fairman, Sanath R. Wijerathna, Nathan R. Kreischer, John LaMacchia, Elizabeth Helmbrecht, Barry S. Cooperman, and Chris Dealwis
Web Release Date: Wed, 9 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800350u

Source: Journal of Medicinal Chemistry | 9 Jul 2008 | 6:00 am CEST

Asymmetric Synthesis of 2,3-Dihydro-2-arylquinazolin-4-ones: Methodology and Application to a Potent Fluorescent Tubulin Inhibitor with Anticancer Activity

Gary M. Chinigo, Mikell Paige, Scott Grindrod, Ernest Hamel, Sivanesan Dakshanamurthy, Maksymilian Chruszcz, Wladek Minor, and Milton L. Brown
Web Release Date: Wed, 9 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800271c

Source: Journal of Medicinal Chemistry | 9 Jul 2008 | 6:00 am CEST

Novel Potent and Selective Bile Acid Derivatives as TGR5 Agonists: Biological Screening, Structure−Activity Relationships, and Molecular Modeling Studies

Hiroyuki Sato, Antonio Macchiarulo, Charles Thomas, Antimo Gioiello, Mizuho Une, Alan F. Hofmann, Régis Saladin, Kristina Schoonjans, Roberto Pellicciari, and Johan Auwerx
Web Release Date: Wed, 9 Jul 2008 00:00:00 EDT (Addition/Correction) DOI: 10.1021/jm8007135

Source: Journal of Medicinal Chemistry | 9 Jul 2008 | 6:00 am CEST

Design, Synthesis, and Biological Evaluation of Antiviral Agents Targeting Flavivirus Envelope Proteins

Ze Li, Mansoora Khaliq, Zhigang Zhou, Carol Beth Post, Richard J. Kuhn, and Mark Cushman
Web Release Date: Wed, 9 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800412d

Source: Journal of Medicinal Chemistry | 9 Jul 2008 | 6:00 am CEST

Book Review of Medicinal Chemistry. An Introduction. Second Edition

Kennerly S. Patrick
Web Release Date: Wed, 9 Jul 2008 00:00:00 EDT (Book Review) DOI: 10.1021/jm800676e

Source: Journal of Medicinal Chemistry | 9 Jul 2008 | 6:00 am CEST

Highly Specific and Broadly Potent Inhibitors of Mammalian Secreted Phospholipases A2

Rob C. Oslund, Nathan Cermak, and Michael H. Gelb
Web Release Date: Tue, 8 Jul 2008 00:00:00 EDT (Brief Article) DOI: 10.1021/jm800422v

Source: Journal of Medicinal Chemistry | 8 Jul 2008 | 6:00 am CEST

Synthesis and Anti-HIV Activity of 4′-Substituted 4′-Thiothymidines: A New Entry Based on Nucleophilic Substitution of the 4′-Acetoxy Group

Kazuhiro Haraguchi, Hisashi Shimada, Hiromichi Tanaka, Takayuki Hamasaki, Masanori Baba, Elizabeth A. Gullen, Ginger E. Dutschman, and Yung-Chi Cheng
Web Release Date: Tue, 8 Jul 2008 00:00:00 EDT (Addition/Correction) DOI: 10.1021/jm8006036

Source: Journal of Medicinal Chemistry | 8 Jul 2008 | 6:00 am CEST

Inhibition of Acetylcholinesterase, β-Amyloid Aggregation, and NMDA Receptors in Alzheimer’s Disease: A Promising Direction for the Multi-target-Directed Ligands Gold Rush

Michela Rosini, Elena Simoni, Manuela Bartolini, Andrea Cavalli, Luisa Ceccarini, Nicoleta Pascu, David W. McClymont, Andrea Tarozzi, Maria L. Bolognesi, Anna Minarini, Vincenzo Tumiatti, Vincenza Andrisano, Ian R. Mellor, and Carlo Melchiorre
Web Release Date: Tue, 8 Jul 2008 00:00:00 EDT (Letter) DOI: 10.1021/jm800577j

Source: Journal of Medicinal Chemistry | 8 Jul 2008 | 6:00 am CEST

Lipid-Conjugated Oligonucleotides via “Click Chemistry” Efficiently Inhibit Hepatitis C Virus Translation

Guilhem Godeau, Cathy Staedel, and Philippe Barthélémy
Web Release Date: Tue, 8 Jul 2008 00:00:00 EDT (Letter) DOI: 10.1021/jm800518u

Source: Journal of Medicinal Chemistry | 8 Jul 2008 | 6:00 am CEST

The Effect of 5-Alkyl Modification on the Biological Activity of Pyrrolo[2,3-d]pyrimidine Containing Classical and Nonclassical Antifolates as Inhibitors of Dihydrofolate Reductase and as Antitumor and/or Antiopportunistic Infection Agents1a–1e

Aleem Gangjee, Hiteshkumar D. Jain, Sherry F. Queener, and Roy L. Kisliuk
Web Release Date: Tue, 8 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800244v

Source: Journal of Medicinal Chemistry | 8 Jul 2008 | 6:00 am CEST

Gold(I)-Mediated Inhibition of Protein Tyrosine Phosphatases: A Detailed in Vitro and Cellular Study

Divya Krishnamurthy, Mark R. Karver, Edoardo Fiorillo, Valeria Orrú, Stephanie M. Stanford, Nunzio Bottini, and Amy M. Barrios
Web Release Date: Tue, 8 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800101w

Source: Journal of Medicinal Chemistry | 8 Jul 2008 | 6:00 am CEST

Discovery of (−)-7-Methyl-2-exo-[3′-(6-[18F]fluoropyridin-2-yl)-5′-pyridinyl]-7-azabicyclo[2.2.1]heptane, a Radiolabeled Antagonist for Cerebral Nicotinic Acetylcholine Receptor (α4β2-nAChR) with Optimal Positron Emission Tomography Imaging Properties

Yongjun Gao, Hiroto Kuwabara, Charles E. Spivak, Yingxian Xiao, Kenneth Kellar, Hayden T. Ravert, Anil Kumar, Mohab Alexander, John Hilton, Dean F. Wong, Robert F. Dannals, and Andrew G. Horti
Web Release Date: Tue, 8 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800323d

Source: Journal of Medicinal Chemistry | 8 Jul 2008 | 6:00 am CEST

Central Metal Determines Pharmacokinetics of Chlorophyll-Derived Xenobiotics

Małgorzata Szczygieł, Krystyna Urbańska, Patrycja Jurecka, Iwona Stawoska, Grażyna Stochel, and Leszek Fiedor
Web Release Date: Tue, 8 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm7016368

Source: Journal of Medicinal Chemistry | 8 Jul 2008 | 6:00 am CEST

Synthesis, Biological Evaluation, and Enzyme Docking Simulations of 1,5-Diarylpyrrole-3-Alkoxyethyl Ethers as Selective Cyclooxygenase-2 Inhibitors Endowed with Anti-inflammatory and Antinociceptive Activity

Maurizio Anzini, Michele Rovini, Andrea Cappelli, Salvatore Vomero, Fabrizio Manetti, Maurizio Botta, Lidia Sautebin, Antonietta Rossi, Carlo Pergola, Carla Ghelardini, Monica Norcini, Antonio Giordani, Francesco Makovec, Paola Anzellotti, Paola Patrignani, and Mariangela Biava
Web Release Date: Fri, 4 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800084s

Source: Journal of Medicinal Chemistry | 4 Jul 2008 | 6:00 am CEST

Inorganic Polyhedral Metallacarborane Inhibitors of HIV Protease: A New Approach to Overcoming Antiviral Resistance

Milan Kožíšek, Petr Cígler, Martin Lepšík, Jindřich Fanfrlík, Pavlína Řezáčová, Jiří Brynda, Jana Pokorná, Jaromír Plešek, Bohumír Grüner, Klára Grantz Šašková, Jana Václavíková, Vladimír Král, and Jan Konvalinka
Web Release Date: Fri, 4 Jul 2008 00:00:00 EDT (Brief Article) DOI: 10.1021/jm8002334

Source: Journal of Medicinal Chemistry | 4 Jul 2008 | 6:00 am CEST

Antitumor Activity of Bis-indole Derivatives1

Aldo Andreani, Silvia Burnelli, Massimiliano Granaiola, Alberto Leoni, Alessandra Locatelli, Rita Morigi, Mirella Rambaldi, Lucilla Varoli, Laura Landi, Cecilia Prata, Michael V. Berridge, Carole Grasso, Heinz-Herbert Fiebig, Gerhard Kelter, Angelika M. Burger, and Mark W. Kunkel
Web Release Date: Fri, 4 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800194k

Source: Journal of Medicinal Chemistry | 4 Jul 2008 | 6:00 am CEST

Design, Synthesis, and Antihepatocellular Carcinoma Activity of Nitric Oxide Releasing Derivatives of Oleanolic Acid

Li Chen, Yihua Zhang, Xiangwen Kong, Edward Lan, Zhangjian Huang, Sixun Peng, Daniel L. Kaufman, and Jide Tian
Web Release Date: Fri, 4 Jul 2008 00:00:00 EDT (Brief Article) DOI: 10.1021/jm800167u

Source: Journal of Medicinal Chemistry | 4 Jul 2008 | 6:00 am CEST

Synthesis, Structure−Activity Relationships, and Biological Profiles of a Quinazolinone Class of Histamine H3 Receptor Inverse Agonists

Tsuyoshi Nagase, Takashi Mizutani, Shiho Ishikawa, Etsuko Sekino, Takahide Sasaki, Takashi Fujimura, Sayaka Ito, Yuko Mitobe, Yasuhisa Miyamoto, Ryo Yoshimoto, Takeshi Tanaka, Akane Ishihara, Norihiro Takenaga, Shigeru Tokita, Takehiro Fukami, and Nagaaki Sato
Web Release Date: Fri, 4 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm8003834

Source: Journal of Medicinal Chemistry | 4 Jul 2008 | 6:00 am CEST

Synthesis of New Arylpiperazinylalkylthiobenzimidazole, Benzothiazole, or Benzoxazole Derivatives as Potent and Selective 5-HT1A Serotonin Receptor Ligands

Maria A. Siracusa, Loredana Salerno, Maria N. Modica, Valeria Pittalà, Giuseppe Romeo, Maria E. Amato, Mateusz Nowak, Andrzej J. Bojarski, Ilario Mereghetti, Alfredo Cagnotto, and Tiziana Mennini
Web Release Date: Fri, 4 Jul 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800176x

Source: Journal of Medicinal Chemistry | 4 Jul 2008 | 6:00 am CEST

The Many Roles for Fluorine in Medicinal Chemistry

William K. Hagmann
Web Release Date: Sat, 21 Jun 2008 00:00:00 EDT (Perspective) DOI: 10.1021/jm800219f

Source: Journal of Medicinal Chemistry | 21 Jun 2008 | 6:00 am CEST

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Web Release Date: Wed, 21 Sep 2005 00:00:00 EDT (Editorial) DOI: 10.1021/jm058265h

Source: Journal of Medicinal Chemistry | 21 Sep 2005 | 6:00 am CEST

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Web Release Date: Wed, 12 May 2004 00:00:00 EDT (null) DOI: 10.1021/jm0400855

Source: Journal of Medicinal Chemistry | 12 May 2004 | 6:00 am CEST

In vitro aldose reductase inhibitory activity of some flavonyl-2,4-thiazolidinediones

Source: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Design, synthesis and preliminary screening of novel 3-(2- N , N -dimethylaminoethylthio) indole derivatives as potential 5-HT 6 receptor ligands

Source: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Butyrylcholinesterase, lipoxygenase inhibiting and antifungal alkaloids from isatis tinctoria

Source: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Xanthine dehydrogenase processes retinol to retinoic acid in human mammary epithelial cells

Source: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Effect of mesoionic 4-phenyl-5-(cinnamoyl)-1,3,4-thiadiazolium-2-phenylamine chloride derivative salts on the activities of the nitric oxide synthase and arginase of Leishmania amazonensis

Source: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Synthesis and evaluation of N-substituted indole-3-carboxamide derivatives as inhibitors of lipid peroxidation and superoxide anion formation

Source: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Microbial and xanthine dehydrogenase inhibitory activity of some flavones

Source: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Design, synthesis, characterization, antibacterial and antifungal activities of a novel class of 5,7-diaryl-4,4-dimethyl-4,5,6,7-tetrahydropyridino[3,4-d]-1,2,3-selenadiazoles

Source: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Novel peptide-based pepsin inhibitors containing an epoxide group

Source: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Brucella suis histidinol dehydrogenase: Synthesis and inhibition studies of substituted N-L-histidinylphenylsulfonyl hydrazide

Source: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Antimicrobial effect by extracts of rhizome of Alpinia officinarum Hance may relate to its inhibition of β-ketoacyl-ACP reductase

Source: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Structural elucidation and biological significance of 2-hydroxy-1-naphthaldehyde derived sulfonamides and their first row d-transition metal chelates

Source: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Some kinetic properties of polyphenol oxidase obtained from dill ( Anethum graveolens )

Source: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Urease inhibitor from Datisca cannabina linn

Source: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Modulation of Anopheles gambiae Epsilon glutathione transferase activity by plant natural products in vitro

Source: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

α-Chymotrypsin inhibition studies on the lignans from Vitex negundo Linn

Source: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Renierol from marine sponge Haliclona.SP.: A natural inhibitor of xanthine oxidase with hypouricemic effects

Source: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Some characteristics of Rabbit muscle phosphofructokinase-1 inhibition by ascorbate

Source: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Investigation of the effects of some sulfonamide derivatives on the activities of glucose-6-phosphate dehydrogenase, 6-phospho gluconate dehydrogenase and glutathione reductase from human erythrocytes

Source: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Prediction of caspase-3 inhibitory activity of 1,3-dioxo-4-methyl-2,3-dihydro-1h-pyrrolo[3,4-c] quinolines: QSAR study

Source: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Synthesis and antimycobacterial activity of 4-[5-(substituted phenyl)-4, 5-dihydro-3-isoxazolyl]-2-methylphenols

Source: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Quantitative structure-activity relationship study on affinity profile of a series of 1,8-naphthyridine antagonists toward bovine adenosine receptors

Source: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Obituary - Professor Jörg Stürzebecher

Source: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Advances in assays of matrix metalloproteinases (MMPs) and their inhibitors

Source: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

A quantitative structure-activity r