1-1
| The View from Inside the Receptor
[Full Article - PDF] |
2-9
| Substituted Xanthines, Pteridinediones, and Related Compounds as Potential Antiinflammatory Agents. Synthesis and Biological Evaluation of Inhibitors of Tumor Necrosis Factor 
Howard B. Cottam,
Hsiencheng Shih,
Lida R. Tehrani,
D. Bruce Wasson, and
Dennis A. Carson
[Full Article - PDF] |
10-18
| Discovery of the Hemifumarate and (-L-Alanyloxy)methyl Ether as Prodrugs of an Antirheumatic Oxindole: Prodrugs for the Enolic OH Group
Ralph P. Robinson,
Lawrence A. Reiter,
Wayne E. Barth,
Anthony M. Campeta,
Kelvin Cooper,
Brian J. Cronin,
Rosalina Destito,
Kathleen M. Donahue,
Fred C. Falkner,
Eugene F. Fiese,
Diane L. Johnson,
Alexander V. Kuperman,
Theodore E. Liston,
Deborah Malloy,
John J. Martin,
David Y. Mitchell,
Frank W. Rusek,
Sheri L. Shamblin, and
Charles F. Wright
[Full Article - PDF] |
19-28
| Conformationally Constrained Analogues of Diacylglycerol. 10. Ultrapotent Protein Kinase C Ligands Based on a Racemic 5-Disubstituted Tetrahydro-2-furanone Template
Rajiv Sharma,
Jeewoo Lee,
Shaomeng Wang,
George W. A. Milne,
Nancy E. Lewin,
Peter M. Blumberg, and
Victor E. Marquez
[Full Article - PDF] |
29-35
| Conformationally Constrained Analogues of Diacylglycerol. 11. Ultrapotent Protein Kinase C Ligands Based on a Chiral 5-Disubstituted Tetrahydro-2-furanone Template
Jeewoo Lee,
Shaomeng Wang,
George W. A. Milne,
Rajiv Sharma,
Nancy E. Lewin,
Peter M. Blumberg, and
Victor E. Marquez
[Full Article - PDF] |
36-45
| Conformationally Constrained Analogues of Diacylglycerol. 12. Ultrapotent Protein Kinase C Ligands Based on a Chiral 4,4-Disubstituted Heptono-1,4-lactone Template
Jeewoo Lee,
Rajiv Sharma,
Shaomeng Wang,
George W. A. Milne,
Nancy E. Lewin,
Zoltan Szallasi,
Peter M. Blumberg,
Clifford George, and
Victor E. Marquez
[Full Article - PDF] |
46-55
| Synthesis and Modeling Studies with Monocyclic Analogues of Mycophenolic Acid
Wayne K. Anderson,
Terri L. Boehm,
Gergely M. Makara, and
R. Thomas Swann
[Full Article - PDF] |
56-65
| Synthesis and Biological Activity of Folic Acid and Methotrexate Analogues Containing L-threo-(2S,4S)-4-Fluoroglutamic Acid and DL-3,3-Difluoroglutamic Acid
Barry P. Hart,
William H. Haile,
Nicholas J. Licato,
Wanda E. Bolanowska,
John J. McGuire, and
James K. Coward
[Full Article - PDF] |
66-72
| Synthesis and Biological Evaluation of DL-4,4-Difluoroglutamic Acid and DL- ,-Difluoromethotrexate
Takashi Tsukamoto,
Tomoya Kitazume,
John J. McGuire, and
James K. Coward
[Full Article - PDF] |
73-85
| Quinazoline Antifolate Thymidylate Synthase Inhibitors: -Linked L-D, D-D, and D-L Dipeptide Analogues of 2-Desamino-2-methyl-N10-propargyl-5,8-dideazafolic Acid (ICI 198583)
Vassilios Bavetsias,
Ann L. Jackman,
Rosemary Kimbell,
William Gibson,
F. Thomas Boyle, and
Graham M. F. Bisset
[Full Article - PDF] |
86-95
| (-)-Arctigenin as a Lead Structure for Inhibitors of Human Immunodeficiency Virus Type-1 Integrase
Eckart Eich,
Heinz Pertz,
Macki Kaloga,
Jutta Schulz,
Mark R. Fesen,
Abhijit Mazumder, and
Yves Pommier
[Full Article - PDF] |
96-108
| Potent Human Immunodeficiency Virus Type 1 Protease Inhibitors That Utilize Noncoded D-Amino Acids as P2/P3 Ligands
Louis N. Jungheim,
Timothy A. Shepherd,
Angela J. Baxter,
Jeffrey Burgess,
Steven D. Hatch,
Penny Lubbehusen,
MaryAnn Wiskerchen, and
Mark A. Muesing
[Full Article - PDF] |
109-119
| Synthesis and Structure-Activity Relationships of Phenylenebis(methylene)- Linked Bis-tetraazamacrocycles That Inhibit Human Immunodeficiency Virus Replication. 2. Effect of Heteroaromatic Linkers on the Activity of Bicyclams
Gary J. Bridger,
Renato T. Skerlj,
Sreenivasan Padmanabhan,
Stephen A. Martellucci,
Geoffrey W. Henson,
Michael J. Abrams,
Heidi C. Joao,
Myriam Witvrouw,
Karen De Vreese,
Rudi Pauwels, and
Erik De Clercq
[Full Article - PDF] |
120-125
| Biarylcarboxylic Acids and -amides: Inhibition of Phosphodiesterase Type IV versus [3H]Rolipram Binding Activity and Their Relationship to Emetic Behavior in the Ferret
Allen J. Duplantier,
Michael S. Biggers,
Robert J. Chambers,
John B. Cheng,
Kelvin Cooper,
David B. Damon,
James F. Eggler,
Kenneth G. Kraus,
Anthony Marfat,
Hiroko Masamune,
Joann S. Pillar,
John T. Shirley,
John P. Umland, and
John W. Watson
[Full Article - PDF] |
126-134
| Binding of Arylpiperazines, (Aryloxy)propanolamines, and Tetrahydropyridylindoles to the 5-HT1A Receptor: Contribution of the Molecular Lipophilicity Potential to Three-Dimensional Quantitative Structure-Affinity Relationship Models
Patrick Gaillard,
Pierre-Alain Carrupt,
Bernard Testa, and
Philippe Schambel
[Full Article - PDF] |
135-142
| Structure-Antigastrin Activity Relationships of New Spiroglumide Amido Acid Derivatives
Francesco Makovec,
Walter Peris,
Sandra Frigerio,
Roberto Giovanetti,
Ornella Letari,
Laura Mennuni, and
Laura Revel
[Full Article - PDF] |
143-148
| 3-Benzisothiazolylpiperazine Derivatives as Potential Atypical Antipsychotic Agents
Harry R. Howard,
John A. Lowe, III,
Thomas F. Seeger,
Patricia A. Seymour,
Stevin H. Zorn,
Patrick R. Maloney,
Frank E. Ewing,
Michael E. Newman,
Anne W. Schmidt,
Jerome S. Furman,
Gwendolyn L. Robinson,
Elisa Jackson,
Celeste Johnson, and
Jean Morrone
[Full Article -
PDF] |
149-157
| Effect of Linking Bridge Modifications on the Antipsychotic Profile of Some Phthalimide and Isoindolinone Derivatives
Mark H. Norman,
Douglas J. Minick, and
Greg C. Rigdon
[Full Article -
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158-175
| High-Affinity Partial Agonist Imidazo[1,5-a]quinoxaline Amides, Carbamates, and Ureas at the -Aminobutyric Acid A/Benzodiazepine Receptor Complex
E. Jon Jacobsen,
Ruth E. TenBrink,
Lindsay S. Stelzer,
Kenneth L. Belonga,
Donald B. Carter,
Haesook K. Im,
Wha Bin Im,
Vimala H. Sethy,
Andy H. Tang,
Philip F. VonVoigtlander, and
James D. Petke
[Full Article -
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176-182
| New  and 5-HT1A Receptor Ligands:  -(Tetralin-1-yl)-n-alkylamine Derivatives
Francesco Berardi,
Nicola A. Colabufo,
Giuseppe Giudice,
Roberto Perrone, and
Vincenzo Tortorella
, Stefano Govoni and
Laura Lucchi
[Full Article -
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183-190
| N-Methyl-D-aspartic Acid Receptor Agonists: Resolution, Absolute Stereochemistry, and Pharmacology of the Enantiomers of 2-Amino-2-(3-hydroxy-5-methyl-4-isoxazolyl)acetic Acid
Ulf Madsen,
Karla Frydenvang,
Bjarke Ebert,
Tommy N. Johansen,
Lotte Brehm, and
Povl Krogsgaard-Larsen
[Full Article -
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191-196
| In Vitro and in Vivo Studies of Benzisoquinoline Ligands for the Brain Synaptic Vesicle Monoamine Transporter
Lihsueh C. Lee,
Thierry Vander Borght,
Phillip S. Sherman,
Kirk A. Frey, and
Michael R. Kilbourn
[Full Article -
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197-206
| Structure-Activity Relationships in a Series of 2(1H)-Quinolones Bearing Different Acidic Function in the 3-Position: 6,7-Dichloro-2(1H)-oxoquinoline-3-phosphonic Acid, a New Potent and Selective AMPA/Kainate Antagonist with Neuroprotective Properties
Patrice Desos,
Jean M. Lepagnol,
Philippe Morain,
Pierre Lestage, and
Alex A. Cordi
[Full Article -
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207-216
| The Squalestatins: Decarboxy and 4-Deoxy Analogues as Potent Squalene Synthase Inhibitors
Chuen Chan,
Daniele Andreotti,
Brian Cox,
Brian W. Dymock,
Julie L. Hutson,
Suzanne E. Keeling,
Alun D. McCarthy,
Panayiotis A. Procopiou,
Barry C. Ross,
Meenu Sareen,
Jan J. Scicinski,
Peter J. Sharratt,
Michael A. Snowden, and
Nigel S. Watson
[Full Article -
PDF] |
217-223
| Design and Synthesis of Non-Peptide Ras CAAX Mimetics as Potent Farnesyltransferase Inhibitors
Yimin Qian,
Andreas Vogt,
Saïd M. Sebti, and
Andrew D. Hamilton
[Full Article -
PDF] |
224-236
| Development of Highly Potent Inhibitors of Ras Farnesyltransferase Possessing Cellular and in Vivo Activity
Katerina Leftheris,
Toni Kline,
Gregory D. Vite,
Young H. Cho,
Rajeev S. Bhide,
Dinesh V. Patel,
Manorama M. Patel,
Robert J. Schmidt,
Harold N. Weller,
Mary L. Andahazy,
Joan M. Carboni,
Johnni L. Gullo-Brown,
Francis Y. F. Lee,
Carol Ricca,
William C. Rose,
Ning Yan,
Mariano Barbacid,
John T. Hunt,
Chester A. Meyers,
Bernd R. Seizinger,
Robert Zahler, and
Veeraswamy Manne
[Full Article -
PDF] |
237-245
| Azole Phenoxy Hydroxyureas as Selective and Orally Active Inhibitors of 5-Lipoxygenase
Michael S. Malamas,
Richard P. Carlson,
David Grimes,
Ralph Howell,
Keith Glaser,
Iwan Gunawan,
James A. Nelson,
Mira Kanzelberger,
Uresh Shah, and
David A. Hartman
[Full Article -
PDF] |
246-252
| Dibenzoxepinone Hydroxylamines and Hydroxamic Acids: Dual Inhibitors of Cyclooxygenase and 5-Lipoxygenase with Potent Topical Antiinflammatory Activity
R. Richard L. Hamer,
John J. Tegeler,
Ellen S. Kurtz,
Richard C. Allen,
Steven C. Bailey,
Mary Ellen Elliott,
Luther Hellyer,
Grover C. Helsley,
Penelope Przekop,
Brian S. Freed,
John White, and
Lawrence L. Martin
[Full Article -
PDF] |
253-266
| Diarylspiro[2.4]heptenes as Orally Active, Highly Selective Cyclooxygenase-2 Inhibitors: Synthesis and Structure-Activity Relationships
Horng-Chih Huang,
James J. Li,
Danny J. Garland,
Timothy S. Chamberlain,
Emily J. Reinhard,
Robert E. Manning,
Karen Seibert,
Carol M. Koboldt,
Susan A. Gregory,
Gary D. Anderson,
Amy W. Veenhuizen,
Yan Zhang,
William E. Perkins,
Earl G. Burton,
J. Nita Cogburn,
Peter C. Isakson, and
David B. Reitz
[Full Article -
PDF] |
267-276
| Tyrosine Kinase Inhibitors. 8. An Unusually Steep Structure-Activity Relationship for Analogues of 4-(3-Bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a Potent Inhibitor of the Epidermal Growth Factor Receptor
Alexander J. Bridges,
Hairong Zhou,
Donna R. Cody,
Gordon W. Rewcastle,
Amy McMichael,
H. D. Hollis Showalter,
David W. Fry,
Alan J. Kraker, and
William A. Denny
[Full Article -
PDF] |
277-284
| Theoretical Study of Inhibition of Adenosine Deaminase by (8R)-Coformycin and (8R)-Deoxycoformycin
Tami J. Marrone,
T. P. Straatsma,
James M. Briggs,
David K. Wilson,
Florante A. Quiocho, and
J. Andrew McCammon
[Full Article -
PDF] |
285-296
| Conformational Analysis of D1 Dopamine Receptor Agonists: Pharmacophore Assessment and Receptor Mapping
David M. Mottola,
Sergei Laiter,
Val J. Watts,
Alexander Tropsha,
Steven D. Wyrick,
David E. Nichols, and
Richard B. Mailman
[Full Article -
PDF] |
297-303
| Studies of Cardiotonic Agents. 8. Synthesis and Biological Activities of Optically Active 6-(4-(Benzylamino)-7-quinazolinyl)-4,5-dihydro-5-methyl- 3(2H)-pyridazinone (KF15232)
Yuji Nomoto,
Haruki Takai,
Tetsuji Ohno,
Ken Nagashima,
Kozo Yao,
Koji Yamada,
Kazuhiro Kubo,
Michio Ichimura,
Akira Mihara, and
Hiroshi Kase
[Full Article -
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304-313
| Cardioselective Antiischemic ATP-Sensitive Potassium Channel Openers. 4. Structure-Activity Studies on Benzopyranylcyanoguanidines: Replacement of the Benzopyran Portion
Karnail S. Atwal,
Francis N. Ferrara,
Charles Z. Ding,
Gary J. Grover,
Paul G. Sleph,
Steven Dzwonczyk,
Anne J. Baird, and
Diane E. Normandin
[Full Article -
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314-322
| Binding of O-Alkyl Derivatives of Serotonin at Human 5-HT1D Receptors
Richard A. Glennon,
Seoung-Soo Hong,
Mikhail Bondarev,
Ho Law,
Malgorzata Dukat,
Suman Rakhit,
Patricia Power,
Ermei Fan,
Diana Kinneau,
Rajender Kamboj,
Milt Teitler,
Katharine Herrick-Davis, and
Carol Smith
[Full Article -
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323-338
| Nonpeptide Angiotensin II Receptor Antagonists: Synthesis, Biological Activities, and Structure-Activity Relationships of Imidazole-5-carboxylic Acids Bearing Alkyl, Alkenyl, and Hydroxyalkyl Substituents at the 4-Position and Their Related Compounds
Hiroaki Yanagisawa,
Yoshiya Amemiya,
Takuro Kanazaki,
Yasuo Shimoji,
Koichi Fujimoto,
Yoshiko Kitahara,
Toshio Sada,
Makoto Mizuno,
Masahiro Ikeda,
Shuichi Miyamoto,
Youji Furukawa, and
Hiroyuki Koike
[Full Article -
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339-341
| Synthesis and Antitumor Evaluation of a Highly Potent Cytotoxic DNA Cross-Linking Polyamine Analogue, 1,12-Diaziridinyl-4,9-diazadodecane
Yanlong Li,
Julie L. Eiseman,
Dorothy L. Sentz,
Faye A. Rogers,
Su-Shu Pan,
Li-Tai Hu,
Merrill J. Egorin, and
Patrick S. Callery
[Full Article -
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342-342
| Computer-Aided Molecular Design. Applications in Agrochemicals, Materials, and Pharmaceuticals Edited by C. Reynolds, M. Holloway, and H. Cox. American Chemical Society, Washington, DC. 1995. x + 428 pp. 15.5 × 23.5 cm. ISBN 0-8412-3160-5. $109.95.
J. Scott Dixon
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342-342
| To See the Obvious. By Arthur J. Birch. In Profiles, Pathways and Dreams Edited by Jeffrey I. Seeman. American Chemical Society, Washington, DC. 1995. xxviii + 269 pp. 15 × 23 cm. ISBN 0-8412-1840-4. $24.95.
Derek H. R. Barton
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