- Melanin-Concentrating
Hormone Receptor 1 Antagonists.
Synthesis and Structure–Activity Relationships of Novel 3-(Aminomethyl)quinolines February 22, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201596hMakoto Kamata, Toshiro Yamashita, Toshihiro Imaeda, Toshio Tanaka, Shinichi Masada, Masahiro Kamaura, Shizuo Kasai, Ryoma Hara, Shigekazu Sasaki, Shiro Takekawa, Asano Asami, Tomoko Kaisho, Nobuhiro Suzuki, Shuntaro Ashina, Hitomi Ogino, Yoshihide Nakano, Yasutaka Nagisa, Koki Kato, Kaneyoshi Kato and Yuji Ishihara
- From the First Selective
Non-Peptide AT2 Receptor Agonist to Structurally Related
Antagonists February 22, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm2015099A. M. S. Murugaiah, Xiongyu Wu, Charlotta Wallinder, A. K. Mahalingam, Yiqian Wan, Christian Sköld, Milad Botros, Marie-Odile Guimond, Advait Joshi, Fred Nyberg, Nicole Gallo-Payet, Anders Hallberg and Mathias Alterman
- A Novel Class of Highly
Potent Irreversible Hepatitis
C Virus NS5B Polymerase Inhibitors February 22, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201322rKevin X. Chen, Charles A. Lesburg, Bancha Vibulbhan, Weiying Yang, Tin-Yau Chan, Srikanth Venkatraman, Francisco Velazquez, Qingbei Zeng, Frank Bennett, Gopinadhan N. Anilkumar, Jose Duca, Yueheng Jiang, Patrick Pinto, Li Wang, Yuhua Huang, Oleg Selyutin, Stephen Gavalas, Haiyan Pu, Sony Agrawal, Boris Feld, Hsueh-Cheng Huang, Cheng Li, Kuo-Chi Cheng, Neng-Yang Shih, Joseph A. Kozlowski, Stuart B. Rosenblum and F. George Njoroge
- Inhibitors of Human Immunodeficiency
Virus Type 1
(HIV-1) Attachment 6. Preclinical and Human Pharmacokinetic Profiling
of BMS-663749, a Phosphonooxymethyl Prodrug of the HIV-1 Attachment
Inhibitor 2-(4-Benzoyl-1-piperazinyl)-1-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)-2-oxoethanone (BMS-488043) February 22, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201218mJohn F. Kadow, Yasutsugu Ueda, Nicholas A. Meanwell, Timothy P. Connolly, Tao Wang, Chung-Pin Chen, Kap-Sun Yeung, Juliang Zhu, John A. Bender, Zhong Yang, Dawn Parker, Pin-Fang Lin, Richard J. Colonno, Marina Mathew, Daniel Morgan, Ming Zheng, Caly Chien and Dennis Grasela
- From a Marine Neuropeptide
to Antimicrobial Pseudopeptides
Containing Aza-β3-Amino Acids: Structure and Activity February 22, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm2011595Mathieu Laurencin, Baptiste Legrand, Emilie Duval, Joël Henry, Michèle Baudy-Floc’h, Céline Zatylny-Gaudin and Arnaud Bondon
- Inhibition of Galactosyltransferases
by a Novel Class
of Donor Analogues February 22, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201154pKarine Descroix, Thomas Pesnot, Yayoi Yoshimura, Sebastian S. Gehrke, Warren Wakarchuk, Monica M. Palcic and Gerd K. Wagner
- Amine Linked Flavonoid
Dimers as Modulators for P-Glycoprotein-Based Multidrug Resistance:
Structure–Activity Relationship and Mechanism of Modulation February 22, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201121bKin-Fai Chan, Iris L. K. Wong, Jason W. Y. Kan, Clare S. W. Yan, Larry M. C. Chow and Tak Hang Chan
- Small Peptide Inhibitors
of Acetyl-Peptide Hydrolase
Having an Uncommon Mechanism of Inhibition and a Stable Bent Conformation February 21, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm2013375A. Sandomenico, A. Russo, G. Palmieri, P. Bergamo, M. Gogliettino, L. Falcigno and M. Ruvo
- Identification and Structure–Activity
Relationships
of a Novel Series of Estrogen Receptor Ligands Based on 7-Thiabicyclo[2.2.1]hept-2-ene-7-oxide February 21, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201556rPengcheng Wang, Jian Min, Jerome C. Nwachukwu, Valerie Cavett, Kathryn E. Carlson, Pu Guo, Manghong Zhu, Yangfan Zheng, Chune Dong, John A. Katzenellenbogen, Kendall W. Nettles and Hai-Bing Zhou
- Binding Affinity Prediction
for Ligands and Receptors Forming Tautomers and Ionization Species:
Inhibition of Mitogen-Activated Protein Kinase-Activated Protein Kinase
2 (MK2) February 17, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201217qSenthil Natesan, Rajesh Subramaniam, Charles Bergeron and Stefan Balaz
- Identification of Binding
Specificity-Determining
Features in Protein Families February 17, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm200979xPeter C. Anderson, Vincent De Sapio, Kevin B. Turner, Sidney P. Elmer, Diana C. Roe and Joseph S. Schoeniger
- Synthesis and Characterization
of Novel 2-Amino-3-benzoylthiophene
Derivatives as Biased Allosteric Agonists and Modulators of the Adenosine
A1 Receptor February 17, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201600eCeline Valant, Luigi Aurelio, Shane M. Devine, Trent D. Ashton, Jonathan M. White, Patrick M. Sexton, Arthur Christopoulos and Peter J. Scammells
- Irreversible Inhibition
of Epidermal Growth Factor
Receptor Activity by 3-Aminopropanamides February 17, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201507xCaterina Carmi, Elena Galvani, Federica Vacondio, Silvia Rivara, Alessio Lodola, Simonetta Russo, Stefania Aiello, Fabrizio Bordi, Gabriele Costantino, Andrea Cavazzoni, Roberta R. Alfieri, Andrea Ardizzoni, Pier Giorgio Petronini and Marco Mor
- Design, Synthesis, and
Biological Evaluation of 1-[(2-Benzyloxyl/alkoxyl)methyl]-5-halo-6-aryluracils
as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with
an Improved Drug Resistance Profile February 17, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201506eXiaowei Wang, Jianfang Zhang, Yang Huang, Ruiping Wang, Liang Zhang, Kang Qiao, Li Li, Chang Liu, Yabo Ouyang, Weisi Xu, Zhili Zhang, Liangren Zhang, Yiming Shao, Shibo Jiang, Liying Ma and Junyi Liu
- Synthesis and Biological
Properties of
Highly Sequence-Specific-Alkylating N-Methylpyrrole–N-Methylimidazole Polyamide Conjugates February 17, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201225zGengo Kashiwazaki, Toshikazu Bando, Tomofumi Yoshidome, Seiji Masui, Toshiki Takagaki, Kaori Hashiya, Ganesh N. Pandian, Junichi Yasuoka, Kazunari Akiyoshi and Hiroshi Sugiyama
- A Click Chemistry Approach
to Pleuromutilin Derivatives,
Part 2: Conjugates with Acyclic Nucleosides and Their Ribosomal Binding
and Antibacterial Activity February 16, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201266bIda Dreier, Surender Kumar, Helle Søndergaard, Maria Louise Rasmussen, Lykke Haastrup Hansen, Nanna Holmgaard List, Jacob Kongsted, Birte Vester and Poul Nielsen
- Radiosynthesis and Evaluation
of an 18F-Labeled
Positron Emission Tomography (PET) Radioligand for Brain Histamine
Subtype-3 Receptors Based on a Nonimidazole 2-Aminoethylbenzofuran
Chemotype February 16, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201690hXiaofeng Bao, Shuiyu Lu, Jeih-San Liow, Sami S. Zoghbi, Kimberly J. Jenko, David T. Clark, Robert L. Gladding, Robert B. Innis and Victor W. Pike
- Gold-Containing Indoles
as Anticancer Agents That
Potentiate the Cytotoxic Effects of Ionizing Radiation February 15, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm2005942Sandra Craig, Lei Gao, Irene Lee, Thomas Gray and Anthony J. Berdis
- Strategies for the Design
of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors: Lessons
from the Development of Seven Representative Paradigms February 15, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm200990cDongyue Li, Peng Zhan, Erik De Clercq and Xinyong Liu
- Fragment-Based and Structure-Guided
Discovery and
Optimization of Rho Kinase Inhibitors February 15, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201289rRongshi Li, Mathew P. Martin, Yan Liu, Binglin Wang, Ronil A. Patel, Jin-Yi Zhu, Nan Sun, Roberta Pireddu, Nicholas J. Lawrence, Jiannong Li, Eric B. Haura, Shen-Shu Sung, Wayne C. Guida, Ernst Schonbrunn and Said M. Sebti
- Substituted 3-(5-Imidazo[2,1-b]thiazolylmethylene)-2-indolinones
and Analogues: Synthesis, Cytotoxic Activity, and Study of the Mechanism
of Action February 15, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm2012694Aldo Andreani, Massimiliano Granaiola, Alessandra Locatelli, Rita Morigi, Mirella Rambaldi, Lucilla Varoli, Natalia Calonghi, Concettina Cappadone, Giovanna Farruggia, Claudio Stefanelli, Lanfranco Masotti, Tam L. Nguyen, Ernest Hamel and Robert H. Shoemaker
- Development of Potent
and Selective Inhibitors of Aldo–Keto Reductase 1C3 (Type 5
17β-Hydroxysteroid Dehydrogenase) Based on N-Phenyl-Aminobenzoates and Their Structure–Activity Relationships February 15, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201547vAdegoke O. Adeniji, Barry M. Twenter, Michael C. Byrns, Yi Jin, Mo Chen, Jeffrey D. Winkler and Trevor M. Penning
- The Power of MMPA and
a Teaching Lesson in Medicinal Chemistry February 15, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm300163yKlaus Müller
- Discovery and Synthesis
of Hydronaphthoquinones as
Novel Proteasome Inhibitors February 14, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201118hYiyu Ge, Aslamuzzaman Kazi, Frank Marsilio, Yunting Luo, Sanjula Jain, Wesley Brooks, Kenyon G. Daniel, Wayne C. Guida, Saïd M. Sebti and Harshani R. Lawrence
- Cyclooxygenase-1-Selective
Inhibitors Based on the
(E)-2′-Des-methyl-sulindac
Sulfide Scaffold February 14, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201528bAndy J. Liedtke, Brenda C. Crews, Cristina M. Daniel, Anna L. Blobaum, Philip J. Kingsley, Kebreab Ghebreselasie and Lawrence J. Marnett
- Chemical Optimization
of New Ligands of the Low-Density Lipoprotein Receptor as Potential
Vectors for Central Nervous System Targeting February 14, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm2014919Jean-Daniel Malcor, Nadine Payrot, Marion David, Aude Faucon, Karima Abouzid, Guillaume Jacquot, Nicolas Floquet, Franck Debarbieux, Geneviève Rougon, Jean Martinez, Michel Khrestchatisky, Patrick Vlieghe and Vincent Lisowski
- Discovery and Development
of Spleen Tyrosine Kinase (SYK) Inhibitors February 14, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201271bRajinder Singh, Esteban S. Masuda and Donald G. Payan
- Oxaphosphinanes: New Therapeutic
Perspectives for
Glioblastoma February 14, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201428aLudovic Clarion, Carine Jacquard, Odile Sainte-Catherine, Séverine Loiseau, Damien Filippini, Marie-Hélène Hirlemann, Jean-Noël Volle, David Virieux, Marc Lecouvey, Jean-Luc Pirat and Norbert Bakalara
- Structure-Based Design
of Potent and Ligand-Efficient
Inhibitors of CTX-M Class A β-Lactamase February 14, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm2014138Derek A. Nichols, Priyadarshini Jaishankar, Wayne Larson, Emmanuel Smith, Guoqing Liu, Racha Beyrouthy, Richard Bonnet, Adam R. Renslo and Yu Chen
- Fused Piperidines as a
Novel Class of Potent and Orally
Available Transient Receptor Potential Melastatin Type 8 (TRPM8) Antagonists February 13, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm2013634Nuria A. Tamayo, Yunxin Bo, Vijay Gore, Vu Ma, Nobuko Nishimura, Phi Tang, Hong Deng, Lana Klionsky, Sonya G. Lehto, Weiya Wang, Brad Youngblood, Jiyun Chen, Tiffany L. Correll, Michael D. Bartberger, Narender R. Gavva and Mark H. Norman
- Update on the Development
of Antagonists of Chemoattractant
Receptor-Homologous Molecule Expressed on Th2 Cells (CRTH2). From
Lead Optimization to Clinical Proof-of-Concept in Asthma and Allergic
Rhinitis February 13, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm2013997Roy Pettipher and Mark Whittaker
- Azaindenoisoquinolines
as Topoisomerase I Inhibitors
and Potential Anticancer Agents: A Systematic Study of
Structure–Activity Relationships February 13, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201512xEvgeny Kiselev, Keli Agama, Yves Pommier and Mark Cushman
- N-Phosphonocarbonylpyrrolidine
Derivatives of Guanine: A New Class of Bi-Substrate Inhibitors of
Human Purine Nucleoside Phosphorylase February 13, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201409uDominik Rejman, Natalya Panova, Pavel Klener, Bokang Maswabi, Radek Pohl and Ivan Rosenberg
- Dual Targeting of Histone
Deacetylase and Topoisomerase II with Novel Bifunctional Inhibitors February 13, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm200799pWilliam Guerrant, Vishal Patil, Joshua C. Canzoneri and Adegboyega K. Oyelere
- New Pyridobenzoxazepine
Derivatives Derived from 5-(4-Methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13): Chemical Synthesis and Pharmacological
Evaluation February 13, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm2013419Jean-François Liégeois, Marine Deville, Sébastien Dilly, Cédric Lamy, Floriane Mangin, Mélissa Résimont and Frank I. Tarazi
- Highly Potent and Selective
Fluorescent Antagonists
of the Human Adenosine A3 Receptor Based on the 1,2,4-Triazolo[4,3-a]quinoxalin-1-one Scaffold February 13, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201722yAndrea J. Vernall, Leigh A. Stoddart, Stephen J. Briddon, Stephen J. Hill and Barrie Kellam
- Triphenylbutanamines:
Kinesin Spindle Protein Inhibitors with in Vivo Antitumor Activity February 13, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201195mFang Wang, James A. D. Good, Oliver Rath, Hung Yi Kristal Kaan, Oliver B. Sutcliffe, Simon P. Mackay and Frank Kozielski
- Dithiocarbamates Strongly
Inhibit Carbonic Anhydrases and Show Antiglaucoma Action in Vivo February 13, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm300031jFabrizio Carta, Mayank Aggarwal, Alfonso Maresca, Andrea Scozzafava, Robert McKenna, Emanuela Masini and Claudiu T. Supuran
- Acylthiourea, Acylurea,
and Acylguanidine Derivatives with Potent Hedgehog Inhibiting Activity February 10, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm2013369Antonio Solinas, Hélène Faure, Hermine Roudaut, Elisabeth Traiffort, Angèle Schoenfelder, André Mann, Fabrizio Manetti, Maurizio Taddei and Martial Ruat
- Identification and Preliminary
Characterization of
a Potent, Safe, and Orally Efficacious Inhibitor of Acyl-CoA:Diacylglycerol
Acyltransferase 1 February 10, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201524gVince S. C. Yeh, David W. A. Beno, Sevan Brodjian, Michael E. Brune, Steven C. Cullen, Brian D. Dayton, Madhup K. Dhaon, Hugh D. Falls, Ju Gao, Nelson Grihalde, Philip Hajduk, T. Matthew Hansen, Andrew S. Judd, Andrew J. King, Russel C. Klix, Kelly J. Larson, Yau Y. Lau, Kennan C. Marsh, Scott W. Mittelstadt, Dan Plata, Michael J. Rozema, Jason A. Segreti, Eric J. Stoner, Martin J. Voorbach, Xiaojun Wang, Xili Xin, Gang Zhao, Christine A. Collins, Bryan F. Cox, Regina M. Reilly, Philip R. Kym and Andrew J. Souers
- “True” AntiandrogensSelective
Non-Ligand-Binding Pocket Disruptors of Androgen Receptor–Coactivator
Interactions: Novel Tools for Prostate Cancer February 10, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201438fLaura Caboni, Gemma K. Kinsella, Fernando Blanco, Darren Fayne, William N. Jagoe, Miriam Carr, D. Clive Williams, Mary J. Meegan and David G. Lloyd
- Synthesis, Anticancer
Activities, and Cellular Uptake Studies of Lipophilic Derivatives
of Doxorubicin Succinate February 10, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201653uBhupender S. Chhikara, Deendayal Mandal and Keykavous Parang
- Identification of Fused-Ring
Alkanoic Acids with Improved
Pharmacokinetic Profiles that Act as G Protein-Coupled Receptor 40/Free
Fatty Acid Receptor 1 Agonists February 10, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm2012968Nobuyuki Negoro, Shinobu Sasaki, Masahiro Ito, Shuji Kitamura, Yoshiyuki Tsujihata, Ryo Ito, Masami Suzuki, Koji Takeuchi, Nobuhiro Suzuki, Junichi Miyazaki, Takashi Santou, Tomoyuki Odani, Naoyuki Kanzaki, Miyuki Funami, Toshimasa Tanaka, Tsuneo Yasuma and Yu Momose
- Testing the Promiscuity
of Commercial Kinase Inhibitors
Against the AGC Kinase Group Using a Split-luciferase Screen February 10, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201265fBenjamin W. Jester, Alicia Gaj, Carolyn D. Shomin, Kurt J. Cox and Indraneel Ghosh
- Rapid Development of Piperidine
Carboxamides as Potent
and Selective Anaplastic Lymphoma Kinase Inhibitors February 9, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201565sMarian C. Bryan, Douglas A. Whittington, Elizabeth M. Doherty, James R. Falsey, Alan C. Cheng, Renee Emkey, Rachael L. Brake and Richard T. Lewis
- Synthesis and Evaluation
of the Cytotoxicities of Tetraindoles: Observation that the 5-Hydroxy
Tetraindole (SK228) Induces G2 Arrest and Apoptosis in
Human Breast Cancer Cells February 9, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm2013425Wen-Shan Li, Chie-Hong Wang, Shengkai Ko, Tzu Ting Chang, Ya Ching Jen, Ching-Fa Yao, Shivaji V. More and Shu-Chuan Jao
- Defining the Mechanism
of Action and Enzymatic Selectivity
of Psammaplin A against Its Epigenetic Targets February 9, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm2016182Matthias G. J. Baud, Thomas Leiser, Patricia Haus, Sharon Samlal, Ai Ching Wong, Robert J. Wood, Vanessa Petrucci, Mekala Gunaratnam, Siobhan M. Hughes, Lakjaya Buluwela, Fabrice Turlais, Stephen Neidle, Franz-Josef Meyer-Almes, Andrew J. P. White and Matthew J. Fuchter
- Contribution of Phosphates
and Adenine to the Potency
of Adenophostins at the IP3 Receptor: Synthesis of All
Possible Bisphosphates of Adenophostin A February 8, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201571pKana M. Sureshan, Andrew M. Riley, Mark P. Thomas, Stephen C. Tovey, Colin W. Taylor and Barry V. L. Potter
- Minimization of Human Relaxin-3
Leading to High-Affinity Analogues with Increased Selectivity for
Relaxin-Family Peptide 3 Receptor (RXFP3) over RXFP1 February 8, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201505pFazel Shabanpoor, Mohammad Akhter Hossain, Philip J. Ryan, Alessia Belgi, Sharon Layfield, Martina Kocan, Suode Zhang, Chrishan S. Samuel, Andrew L. Gundlach, Ross A.D. Bathgate, Frances Separovic and John D. Wade
- Pyridone Methylsulfone
Hydroxamate LpxC Inhibitors for the Treatment of Serious Gram-Negative
Infections February 8, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm2014875Justin I. Montgomery, Matthew F. Brown, Usa Reilly, Loren M. Price, Joseph A. Abramite, Joel Arcari, Rose Barham, Ye Che, Jinshan Michael Chen, Seung Won Chung, Elizabeth M. Collantes, Charlene Desbonnet, Matthew Doroski, Jonathan Doty, Juntyma J. Engtrakul, Thomas M. Harris, Michael Huband, John D. Knafels, Karen L. Leach, Shenping Liu, Anthony Marfat, Laura McAllister, Eric McElroy, Carol A. Menard, Mark Mitton-Fry, Lisa Mullins, Mark C. Noe, John O’Donnell, Robert Oliver, Joseph Penzien, Mark Plummer, Veerabahu Shanmugasundaram, Christy Thoma, Andrew P. Tomaras, Daniel P. Uccello, Alfin Vaz and Donn G. Wishka
- Aberrant Cyclization Affords
a C-6 Modified Cyclic Adenosine 5′-Diphosphoribose Analogue
with Biological Activity in Jurkat T Cells February 8, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201127yChristelle Moreau, Tanja Kirchberger, Bo Zhang, Mark P. Thomas, Karin Weber, Andreas H. Guse and Barry V. L. Potter
- 3-Aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-one: A Novel Template
for the Design of Highly Selective
A2B Adenosine Receptor Antagonists February 7, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201177bSabrina Taliani, Isabella Pugliesi, Elisabetta Barresi, Francesca Simorini, Silvia Salerno, Concettina La Motta, Anna Maria Marini, Barbara Cosimelli, Sandro Cosconati, Salvatore Di Maro, Luciana Marinelli, Simona Daniele, Maria Letizia Trincavelli, Giovanni Greco, Ettore Novellino, Claudia Martini and Federico Da Settimo
- Structure–Activity
Relationship of Novel Menaquinone-4 Analogues: Modification of the
Side Chain Affects their Biological Activities February 7, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm2013166Yoshitomo Suhara, Norika Hanada, Takashi Okitsu, Miho Sakai, Masato Watanabe, Kimie Nakagawa, Akimori Wada, Kazuyoshi Takeda, Kazuhiko Takahashi, Hiroaki Tokiwa and Toshio Okano
- A Tribute to Joseph G.
Cannon, 1926–2011 February 6, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm300081mJohn L. Neumeyer
- Synthesis and Biological
Activity of 6-Substituted
Pyrrolo[2,3-d]pyrimidine Thienoyl Regioisomers as
Inhibitors of de Novo Purine Biosynthesis with Selectivity for Cellular
Uptake by High Affinity Folate Receptors and the Proton-Coupled Folate
Transporter over the Reduced Folate Carrier February 3, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201688nLei Wang, Christina Cherian, Sita Kugel Desmoulin, Shermaine Mitchell-Ryan, Zhanjun Hou, Larry H. Matherly and Aleem Gangjee
- 5-Imino-1,2,4-Thiadiazoles:
First Small Molecules
As Substrate Competitive Inhibitors of Glycogen Synthase Kinase 3 February 3, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201463vValle Palomo, Daniel I. Perez, Concepcion Perez, Jose A. Morales-Garcia, Ignacio Soteras, Sandra Alonso-Gil, Arantxa Encinas, Ana Castro, Nuria E. Campillo, Ana Perez-Castillo, Carmen Gil and Ana Martinez
- Homobivalent Ligands of
the Atypical Antipsychotic
Clozapine: Design, Synthesis, and Pharmacological Evaluation February 2, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201420sFiona M. McRobb, Ian T. Crosby, Elizabeth Yuriev, J. Robert Lane and Ben Capuano
- Correction to Malaria-Infected
Mice Are Completely Cured by One 6 mg/kg Oral Dose of a New Monomeric
Trioxane Sulfide Combined with Mefloquine February 2, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm300104mRachel D. Slack, Bryan T. Mott, Lauren E. Woodard, Abhai Tripathi, David Sullivan, Elizabeth Nenortas, Sonya C. T. Girdwood, Theresa A. Shapiro and Gary H. Posner
- 1,4-Dioxane, a Suitable
Scaffold for the Development
of Novel M3 Muscarinic Receptor Antagonists February 2, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm2013216Fabio Del Bello, Elisabetta Barocelli, Simona Bertoni, Alessandro Bonifazi, Mercedes Camalli, Gaetano Campi, Mario Giannella, Rosanna Matucci, Marta Nesi, Maria Pigini, Wilma Quaglia and Alessandro Piergentili
- Exploring Activity Cliffs
in Medicinal Chemistry January 27, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201706bDagmar Stumpfe and Jürgen Bajorath
- Discovery of 1,2,4-Triazine
Derivatives as Adenosine
A2A Antagonists using Structure Based Drug Design January 27, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201376wMiles Congreve, Stephen P. Andrews, Andrew S. Doré, Kaspar Hollenstein, Edward Hurrell, Christopher J. Langmead, Jonathan S. Mason, Irene W. Ng, Benjamin Tehan, Andrei Zhukov, Malcolm Weir and Fiona H. Marshall
- Molecular Determinants
of AcrB-Mediated Bacterial
Efflux Implications for Drug Discovery January 27, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201275dJohn I. Manchester, Ed T. Buurman, Gregory S. Bisacchi and Robert E. McLaughlin
- Nucleoside, Nucleotide,
and Non-Nucleoside
Inhibitors of Hepatitis C Virus NS5B RNA-Dependent RNA-Polymerase January 23, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201384jMichael J. Sofia, Wonsuk Chang, Phillip A. Furman, Ralph T. Mosley and Bruce S. Ross
- Avenues for the Development
of Therapeutics That Target
Trace Amine Associated Receptor 1 (TAAR1) January 20, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201437tGregory M. Miller
- Discovery of Inhibitors
of Soluble Epoxide
Hydrolase: A Target with Multiple Potential Therapeutic Indications January 17, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201468jHong C. Shen and Bruce D. Hammock
- Oxadiazoles in Medicinal
Chemistry January 13, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm2013248Jonas Boström, Anders Hogner, Antonio Llinàs, Eric Wellner and Alleyn T. Plowright
- Rational Approaches to
Improving Selectivity
in Drug Design January 12, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm2010332David J. Huggins, Woody Sherman and Bruce Tidor
- Allosteric Modulation
of Seven Transmembrane Spanning
Receptors: Theory, Practice, and Opportunities for Central Nervous
System Drug Discovery January 6, 2012Journal of Medicinal ChemistryDOI: 10.1021/jm201139rBruce J. Melancon, Corey R. Hopkins, Michael R. Wood, Kyle A. Emmitte, Colleen M. Niswender, Arthur Christopoulos, P. Jeffrey Conn and Craig W. Lindsley
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Richard Suder, CFA, CFP®
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