COMMUNICATIONS TO THE EDITOR
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3551-3556
| (Z,Z)-2,7-Bis(4-amidinobenzylidene)cycloheptan-1-one: Identification of a Highly Active Inhibitor of Blood Coagulation Factor Xa
Kenneth J. Shaw,
William J. Guilford,
Jerry L. Dallas,
Sunil K. Koovakkaat,
Margaret A. McCarrick,
Amy Liang,
David R. Light, and
Michael M. Morrissey
[Full Article -
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3557-3562
| Discovery of N-[2-[5-[Amino(imino)methyl]-2-hydroxyphenoxy]-3,5-difluoro- 6-[3-(4,5-dihydro-1-methyl-1H-imidazol-2-yl)phenoxy]pyridin-4-yl]-N-methylglycine (ZK-807834): A Potent, Selective, and Orally Active Inhibitor of the Blood Coagulation Enzyme Factor Xa
Gary B. Phillips,
Brad O. Buckman,
David D. Davey,
Keith A. Eagen,
William J. Guilford,
Josephine Hinchman,
Elena Ho,
Sunil Koovakkat,
Amy Liang,
David R. Light,
Raju Mohan,
Howard P. Ng,
Joseph M. Post,
Kenneth J. Shaw,
Dave Smith,
Babu Subramanyam,
Mark E. Sullivan,
Lan Trinh,
Ron Vergona,
Janette Walters,
Kathy White,
Marc Whitlow,
Shung Wu,
Wei Xu, and
Michael M. Morrissey
[Full Article -
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3563-3567
| Conformationally Constrained 1,3-Diamino Ketones: A Series of Potent Inhibitors of the Cysteine Protease Cathepsin K
Robert W. Marquis,
Dennis S. Yamashita,
Yu Ru,
Stephen M. LoCastro,
Hye-Ja Oh,
Karl F. Erhard,
Renee L. DesJarlais,
Martha S. Head,
Ward W. Smith,
Baoguang Zhao,
Cheryl A. Janson,
Sherin S. Abdel-Meguid,
Thaddeus A. Tomaszek,
Mark A. Levy, and
Daniel F. Veber
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3568-3571
| Discovery of Potent, Achiral Matrix Metalloproteinase Inhibitors
Stanislaw Pikul,
Kelly L. McDow Dunham,
Neil G. Almstead,
Biswanath De,
Michael G. Natchus,
Melanie V. Anastasio,
Sara J. McPhail,
Catherine E. Snider,
Yetunde O. Taiwo,
Timothy Rydel,
C. Michelle Dunaway,
Fei Gu, and
Glen E. Mieling
[Full Article -
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ARTICLES
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3572-3581
| Prodrugs of Anthracyclines for Use in Antibody-Directed Enzyme Prodrug Therapy
Jean-Claude Florent,
Xia Dong,
Gilbert Gaudel,
Sofia Mitaku,
Claude Monneret,
Jean-Pierre Gesson,
Jean-Claude Jacquesy,
Martine Mondon,
Brigitte Renoux,
Solo Andrianomenjanahary,
Sylvie Michel,
Michel Koch,
François Tillequin,
Manfred Gerken,
Joerg Czech,
Rainer Straub, and
Klaus Bosslet
[Full Article -
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3582-3595
| ATP-Citrate Lyase as a Target for Hypolipidemic Intervention. 2. Synthesis and Evaluation of (3R*,5S*)- -Substituted-3-carboxy-3,5-dihydroxyalkanoic Acids and Their -Lactone Prodrugs as Inhibitors of the Enzyme in Vitro and in Vivo
Andrew D. Gribble,
Robert J. Ife,
Antony Shaw,
David McNair,
Christine E. Novelli,
Susan Bakewell,
Virendra P. Shah,
Roland E. Dolle,
Pieter H. Groot,
Nigel Pearce,
John Yates,
David Tew,
Helen Boyd,
Stephen Ashman,
Drake S. Eggleston,
R. Curtis Haltiwanger, and
George Okafo
[Full Article -
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3596-3608
| Classical/Nonclassical Hybrid Cannabinoids: Southern Aliphatic Chain-Functionalized C-6 Methyl, Ethyl, and Propyl Analogues
David J. Drake,
Rader S. Jensen,
Jakob Busch-Petersen,
Joel K. Kawakami,
M. Concepcion Fernandez-Garcia,
Pusheng Fan,
Alexandros Makriyannis, and
Marcus A. Tius
[Full Article -
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3609-3623
| Derivation of a Three-Dimensional Pharmacophore Model of Substance P Antagonists Bound to the Neurokinin-1 Receptor
Yasuo Takeuchi,
E. F. Berkley Shands,
Denise D. Beusen, and
Garland R. Marshall
[Full Article -
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3624-3634
| 2-[N-Acylamino(C1-C3)alkyl]indoles as MT1 Melatonin Receptor Partial Agonists, Antagonists, and Putative Inverse Agonists
Gilberto Spadoni,
Cesarino Balsamini,
Annalida Bedini,
Giuseppe Diamantini,
Barbara Di Giacomo,
Andrea Tontini, and
Giorgio Tarzia
, Marco Mor,
Pier Vincenzo Plazzi, and
Silvia Rivara
, Romolo Nonno,
Marilou Pannacci,
Valeria Lucini,
Franco Fraschini, and
Bojidar Michaylov Stankov
[Full Article -
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3635-3644
| 2-Deoxy Derivative Is a Partial Agonist of the Intracellular Messenger Inositol 3,4,5,6-Tetrakisphosphate in the Epithelial Cell Line T84
Marco T. Rudolf,
Wen-hong Li,
Nora Wolfson,
Alexis E. Traynor-Kaplan, and
Carsten Schultz
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3645-3654
| Synthesis and Antitumor Activity of 4-Aminomethylthioxanthenone and 5-Aminomethylbenzothiopyranoindazole Derivatives
Robert B. Perni,
Mark P. Wentland,
Jianhua I. Huang,
Ronald G. Powles,
Suzanne Aldous,
Kristina M. Klingbeil,
A. Danielle Peverly,
Ronald G. Robinson,
Thomas H. Corbett,
Julie L. Jones,
Kenneth C. Mattes,
James B. Rake, and
Susan A. Coughlin
[Full Article -
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3655-3663
| Biologically Active Oligodeoxyribonucleotides. 5. 5'-End-Substituted d(TGGGAG) Possesses Anti-Human Immunodeficiency Virus Type 1 Activity by Forming a G-Quadruplex Structure
Hitoshi Hotoda,
Makoto Koizumi,
Rika Koga,
Masakatsu Kaneko,
Kenji Momota,
Toshinori Ohmine,
Hidehiko Furukawa,
Toshinori Agatsuma,
Takashi Nishigaki,
Junko Sone,
Shinya Tsutsumi,
Toshiyuki Kosaka,
Koji Abe,
Satoshi Kimura, and
Kaoru Shimada
[Full Article -
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3664-3674
| Rational Design, Synthesis, and X-ray Structure of Selective Noncovalent Thrombin Inhibitors
Jürgen Wagner,
Jörg Kallen,
Claus Ehrhardt,
Jean-Pierre Evenou, and
Dieter Wagner
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3675-3683
| 2-Iminopyrrolidines as Potent and Selective Inhibitors of Human Inducible Nitric Oxide Synthase
Timothy J. Hagen,
Arija A. Bergmanis,
Steven W. Kramer,
Kam F. Fok,
Albert E. Schmelzer,
Barnett S. Pitzele,
Lydia Swenton,
Gina M. Jerome,
Christine M. Kornmeier,
William M. Moore,
Linda F. Branson,
Jane R. Connor,
Pamela T. Manning,
Mark G. Currie, and
E. Ann Hallinan
[Full Article -
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3684-3689
| Reactions of Melatonin and Related Indoles with Free Radicals: A Computational Study
Adrián G. Turjanski,
Ruth E. Rosenstein, and
Darío A. Estrin
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3690-3698
| 2-, 5-, and 6-Halo-3-(2(S)-azetidinylmethoxy)pyridines: Synthesis, Affinity for Nicotinic Acetylcholine Receptors, and Molecular Modeling
Andrei O. Koren,
Andrew G. Horti,
Alexey G. Mukhin,
Daniela Gündisch,
Alane S. Kimes,
Robert F. Dannals, and
Edythe D. London
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3699-3704
| A New Series of Highly Potent Growth Hormone-Releasing Peptides Derived from Ipamorelin
Michael Ankersen,
Nils L. Johansen,
Kjeld Madsen,
Birgit S. Hansen,
Kirsten Raun,
Karin Kramer Nielsen,
Henning Th gersen,
Thomas K. Hansen,
Bernd Peschke,
Jesper Lau,
Behrend F. Lundt, and
Peter H. Andersen
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3705-3714
| Novel Orally Active Growth Hormone Secretagogues
Thomas K. Hansen,
Michael Ankersen,
Birgit S. Hansen,
Kirsten Raun,
Karin K. Nielsen,
Jesper Lau,
Bernd Peschke,
Behrend F. Lundt,
Henning Th gersen,
Nils L. Johansen,
Kjeld Madsen, and
Peter H. Andersen
[Full Article -
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3715-3726
| Synthesis and Biological Evaluation of 2-Acyl Analogues of Paclitaxel (Taxol)
David G. I. Kingston,
Ashok G. Chaudhary,
Mahendra D. Chordia,
Milind Gharpure,
A. A. Leslie Gunatilaka,
Paul I. Higgs,
John M. Rimoldi,
Lakshman Samala, and
Prakash G. Jagtap
, Paraskevi Giannakakou
, Yuan Q. Jiang,
Chii M. Lin, and
Ernest Hamel
, Byron H. Long,
Craig R. Fairchild, and
Kathy A. Johnston
[Full Article -
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3727-3735
| Piperazinyl Oxazolidinone Antibacterial Agents Containing a Pyridine, Diazene, or Triazene Heteroaromatic Ring
John A. Tucker,
Debra A. Allwine,
Kevin C. Grega,
Michael R. Barbachyn,
Jennifer L. Klock,
Jenifer L. Adamski,
Steven J. Brickner,
Douglas K. Hutchinson,
Charles W. Ford,
Gary E. Zurenko,
Robert A. Conradi,
Phillip S. Burton, and
Randy M. Jensen
[Full Article -
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3736-3747
| Bicyclic Acylguanidine Na+/H+ Antiporter Inhibitors
Manfred Baumgarth,
Norbert Beier, and
Rolf Gericke
[Full Article - PDF] |
NOTES
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3748-3752
| Anthracene-9,10-diones as Potential Anticancer Agents: Bacterial Mutation Studies of Amido-Substituted Derivatives Reveal an Unexpected Lack of Mutagenicity
Stanley Venitt,
Christopher Crofton-Sleigh,
Mavis Agbandje,
Terence C. Jenkins, and
Stephen Neidle
[Full Article -
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3753-3757
| Synthesis and Characterization of Heteroarotinoids Demonstrate Structure Specificity Relationships
Doris M. Benbrook,
Shankar Subramanian,
Jonathan B. Gale,
Shengquan Liu,
Chad W. Brown,
Marcus F. Boehm, and
K. Darrell Berlin
[Full Article - PDF] |
BOOK REVIEWS
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3758-3758
| A Complete Introduction to Modern NMR Spectroscopy By Roger S. Macomber. Wiley Interscience, New York, NY. 1998. xvii + 382 pp. 21.5 × 28 cm. ISBN 0-471-15736-8. $49.95.
Horacio F. Olivo
[Full Article - PDF] |
3758-3758
| Receptor-Based Drug Design Edited by Paul Leff. Marcel Dekker, Inc., New York. 1998. xi + 382 pp. 16 × 23 cm. ISBN 0-8247-0162-3. $175.00.
Roger M. Pinder
[Full Article - PDF] |