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ChemInform Abstract: The Medicinal Chemists


Toolbox: An Analysis of Reactions Used in the
Pursuit of Drug Candidates

Article in Journal of Medicinal Chemistry May 2011


DOI: 10.1021/jm200187y Source: PubMed

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2 authors:

Stephen Roughley Allan M Jordan


Vernalis Cancer Research UK Manchester Institute
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May 26, 2011
Volume 54, Issue 10
Pages 3451-3674
1. The Medicinal Chemists Toolbox: An Analysis of Reactions Used in the Pursuit of Drug
Candidates
Stephen D. Roughley, Allan M. Jordan
Journal of Medicinal Chemistry 2011 54 (10), 3451-3479
2. Design, Synthesis, Radiolabeling, and in Vitro and in Vivo Evaluation of Bridgehead
Iodinated Analogues of N-{2-[4-(2-Methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-
yl)cyclohexanecarboxamide (WAY-100635) as Potential SPECT Ligands for the 5-HT1A
Receptor
Rana Al Hussainy, Joost Verbeek, Dion van der Born, Anton H. Braker, Jos e E. Leysen, Remco
J. Knol, Jan Booij, J. (Koos) D. M. Herscheid
Journal of Medicinal Chemistry 2011 54 (10), 3480-3491
3. Two-Step Synthesis of Novel, Bioactive Derivatives of the Ubiquitous Cofactor
Nicotinamide Adenine Dinucleotide (NAD)
Thomas Pesnot, Julia Kempter, J rg Schemies, Giulia Pergolizzi, Urszula Uciechowska, Tobias
Rumpf, Wolfgang Sippl, Manfred Jung, Gerd K. Wagner
Journal of Medicinal Chemistry 2011 54 (10), 3492-3499
4. Selective Depletion of Neuropathy-Related Antibodies from Human Serum by Monolithic
Affinity Columns Containing Ganglioside Mimics
Kishore K. R. Tetala, Astrid P. Heikema, Aliaksei V. Pukin, Carel A. G. M. Weijers, Anne P. Tio-
Gillen, Michel Gilbert, Hubert P. Endtz, Alex van Belkum, Han Zuilhof, Gerben M. Visser, Bart C.
Jacobs, Teris A. van Beek
Journal of Medicinal Chemistry 2011 54 (10), 3500-3505
5. Biomimetic Syntheses and Antiproliferative Activities of Racemic, Natural (), and
Unnnatural (+) Glyceollin I
Rahul S. Khupse, Jeffrey G. Sarver, Jill A. Trendel, Nicole R. Bearss, Michael D. Reese, Thomas
E. Wiese, Stephen M. Boue, Matthew E. Burow, Thomas E. Cleveland, Deepak Bhatnagar, Paul
W. Erhardt
Journal of Medicinal Chemistry 2011 54 (10), 3506-3523
6. Development of Amidine-Based Sphingosine Kinase 1 Nanomolar Inhibitors and
Reduction of Sphingosine 1-Phosphate in Human Leukemia Cells
Andrew J. Kennedy, Thomas P. Mathews, Yugesh Kharel, Saundra D. Field, Morgan L. Moyer,
James E. East, Joseph D. Houck, Kevin R. Lynch, Timothy L. Macdonald
Journal of Medicinal Chemistry 2011 54 (10), 3524-3548
7. Potent and Selective Phosphopeptide Mimetic Prodrugs Targeted to the Src Homology 2
(SH2) Domain of Signal Transducer and Activator of Transcription 3
Pijus K. Mandal, Fengqin Gao, Zhen Lu, Zhiyong Ren, Rajagopal Ramesh, J. Sanderson
Birtwistle, Kumaralal K. Kaluarachchi, Xiaomin Chen, Robert C. Bast Jr., Warren S. Liao, John S.
McMurray
Journal of Medicinal Chemistry 2011 54 (10), 3549-3563
8. SHAFTS: A Hybrid Approach for 3D Molecular Similarity Calculation. 2. Prospective Case
Study in the Discovery of Diverse p90 Ribosomal S6 Protein Kinase 2 Inhibitors To
Suppress Cell Migration
Weiqiang Lu, Xiaofeng Liu, Xianwen Cao, Mengzhu Xue, Kangdong Liu, Zhenjiang Zhao, Xu
Shen, Hualiang Jiang, Yufang Xu, Jin Huang, Honglin Li
Journal of Medicinal Chemistry 2011 54 (10), 3564-3574
9. Structure of Estradiol Metal Chelate and Estrogen Receptor Complex: The Basis for
Designing a New Class of Selective Estrogen Receptor Modulators
Min-Jun Li, Harry M. Greenblatt, Orly Dym, Shira Albeck, Adi Pais, Chidambaram Gunanathan,
David Milstein, Hadassa Degani, Joel L. Sussman
Journal of Medicinal Chemistry 2011 54 (10), 3575-3580
10. N-(3-Fluoro-4-(4-(2-methoxy or 2,3-dichlorophenyl)piperazine-1-yl)butyl)arylcarboxamides
as Selective Dopamine D3 Receptor Ligands: Critical Role of the Carboxamide Linker for
D3 Receptor Selectivity
Ashwini K. Banala, Benjamin A. Levy, Sameer S. Khatri, Cheryse A. Furman, Rebecca A. Roof,
Yogesh Mishra, Suzy A. Griffin, David R. Sibley, Robert R. Luedtke, Amy Hauck Newman
Journal of Medicinal Chemistry 2011 54 (10), 3581-3594
11. Synthesis, StructureActivity Relationship, and Antimalarial Activity of Ureas and
Thioureas of 15-Membered Azalides
Mirjana Bukvi Kraja i , Mihaela Peri , Kirsten S. Smith, Zrinka Ivezi Sch nfeld, Dinko iher,
Andrea Fajdeti , Nedjeljko Kujund i , Wolfgang Sch nfeld, Goran Landek, Jasna Padovan,
Dubravko Jeli , Arba Ager, Wilbur K. Milhous, William Ellis, Radan Spaventi, Colin Ohrt
Journal of Medicinal Chemistry 2011 54 (10), 3595-3605
12. Synthesis and Evaluation of Hydrophilic Linkers for AntibodyMaytansinoid Conjugates
Robert Y. Zhao, Sharon D. Wilhelm, Charlene Audette, Gregory Jones, Barbara A. Leece,
Alexandru C. Lazar, Victor S. Goldmacher, Rajeeva Singh, Yelena Kovtun, Wayne C. Widdison,
John M. Lambert, Ravi V. J. Chari
Journal of Medicinal Chemistry 2011 54 (10), 3606-3623
13. 3-Trifluoromethylquinoxaline N,N-Dioxides as Anti-Trypanosomatid Agents. Identification
of Optimal Anti-T. cruzi Agents and Mechanism of Action Studies
Diego Benitez, Mauricio Cabrera, Paola Hern ndez, Luc a Boiani, Mar a L. Lavaggi, Rossanna
Di Maio, Gloria Yaluff, Elva Serna, Susana Torres, Mar a E. Ferreira, Ninfa Vera de Bilbao,
Enrique Torres, Silvia P rez-Silanes, Beatriz Solano, Elsa Moreno, Ignacio Aldana, Adela L pez
de Cer in, Hugo Cerecetto, Mercedes Gonz lez, Antonio Monge
Journal of Medicinal Chemistry 2011 54 (10), 3624-3636
14. Enone and ChalconeChloroquinoline Hybrid Analogues: In Silico Guided Design,
Synthesis, Antiplasmodial Activity, in Vitro Metabolism, and Mechanistic Studies
Eric M. Guantai, Kanyile Ncokazi, Timothy J. Egan, Jiri Gut, Philip J. Rosenthal, Ravi
Bhampidipati, Anitha Kopinathan, Peter J. Smith, Kelly Chibale
Journal of Medicinal Chemistry 2011 54 (10), 3637-3649
15. Discovery of Dual Target Inhibitors against Cyclooxygenases and Leukotriene A4
Hydrolyase
Zheng Chen, Yiran Wu, Ying Liu, Suijia Yang, Yunjie Chen, Luhua Lai
Journal of Medicinal Chemistry 2011 54 (10), 3650-3660
16. Potent, Selective, and Orally Available Benzoisothiazolone Phosphomannose Isomerase
Inhibitors as Probes for Congenital Disorder of Glycosylation Ia
Russell Dahl, Yalda Bravo, Vandana Sharma, Mie Ichikawa, Raveendra-Panickar Dhanya,
Michael Hedrick, Brock Brown, Justin Rascon, Michael Vicchiarelli, Arianna Mangravita-Novo, Li
Yang, Derek Stonich, Ying Su, Layton H. Smith, Eduard Sergienko, Hudson H. Freeze, Nicholas
D. P. Cosford
Journal of Medicinal Chemistry 2011 54 (10), 3661-3668
17. Novel Potent and Selective Ligands: Evaluation of Their Agonist and Antagonist
Properties
Agostino Marrazzo, Enrique J. Cobos, Carmela Parenti, Giuseppina Aric , Giuseppina Marrazzo,
Simone Ronsisvalle, Lorella Pasquinucci, Orazio Prezzavento, Nicola A. Colabufo,
Marialessandra Contino, Luis G. Gonz lez, Giovanna M. Scoto, Giuseppe Ronsisvalle
Journal of Medicinal Chemistry 2011 54 (10), 3669-3673

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