Semisynthetic Maytansine Analogues for the Targeted Treatment of Cancer (Ohne Sprachangabe)

In: Journal of medicinal chemistry   ;  49 ,  14  ;  2006
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Inhaltsverzeichnis – Band 49, Ausgabe 14

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3999
Approaches to Antiobesity Therapy. An Introduction
Bishop, Michael J. | 2006
4001
Obesity:  The Disease
Bray, George A. | 2006
4008
CB1Cannabinoid Receptor Antagonists for Treatment of Obesity and Prevention of Comorbid Metabolic Disorders
Antel, Jochen / Gregory, Peter C. / Nordheim, Ulrich | 2006
4017
Melanin-Concentrating Hormone-1 Receptor Antagonists for the Treatment of Obesity
Handlon, Anthony L. / Zhou, Huiqiang | 2006
4023
5-Hydroxytryptamine 2C (5-HT2C) Receptor Agonists as Potential Antiobesity Agents
Nilsson, Björn M. | 2006
4035
Melanocortin-4 Receptor (MC4R) Agonists for the Treatment of Obesity
Nargund, Ravi P. / Strack, Alison M. / Fong, Tung M. | 2006
4044
Discovery of Novel Triazole-Based Opioid Receptor Antagonists
Zhang, Qiang / Keenan, Susan M. / Peng, Youyi / Nair, Anil C. / Yu, Seong Jae / Howells, Richard D. / Welsh, William J. | 2006
4048
Development of Peptidic Dopamine Transporter Inhibitors via Aromatic Modification-Mediated Conformational Restriction
Ding, Jinguo / Shi, Jiahao / Cui, Dafu / Xu, Linfeng / Duan, Shuhui / Guo, Lihe / Fei, Jian | 2006
4052
Toward Orthopoxvirus Countermeasures:  A Novel Heteromorphic Nucleoside of Unusual Structure
Fan, Xuesen / Zhang, Xinying / Zhou, Longhu / Keith, Kathy A. / Prichard, Mark N. / Kern, Earl R. / Torrence, Paul F. | 2006
4055
Discovery of Potent and Orally Available Malonyl-CoA Decarboxylase Inhibitors as Cardioprotective Agents
Cheng, Jie-Fei / Huang, Yujin / Penuliar, Richard / Nishimoto, Masahiro / Liu, Larry / Arrhenius, Thomas / Yang, Guang / O'Leary, Eoin / Barbosa, Miguel / Barr, Rick et al. | 2006
4059
FK506-Binding Protein Ligands:  Structure-Based Design, Synthesis, and Neurotrophic/Neuroprotective Properties of Substituted 5,5-Dimethyl-2-(4-thiazolidine)carboxylates
Zhao, Liqin / Huang, Wei / Liu, Hongying / Wang, Lili / Zhong, Wu / Xiao, Junhai / Hu, Yuandong / Li, Song | 2006
4072
Design and Synthesis of the First Generation of Dithiolane Thiazolidinedione- and Phenylacetic Acid-Based PPARγ Agonists
Chittiboyina, Amar G. / Venkatraman, Meenakshi S. / Mizuno, Cassia S. / Desai, Prashant V. / Patny, Akshay / Benson, Stephen C. / Ho, Christopher I. / Kurtz, Theodore W. / Pershadsingh, Harrihar A. / Avery, Mitchell A. | 2006
4072
Design and Synthesis of the First Generation of Dithiolane Thiazolidinedione- and Phenylacetic Acid-Based PPARgamma Agonists
Chittiboyina, A. G. / Venkatraman, M. S. / Mizuno, C. S. / Desai, P. V. / Patny, A. / Benson, S. C. / Ho, C. I. / Kurtz, T. W. / Pershadsingh, H. A. / Avery, M. A. | 2006
4085
Pharmacophore Based Receptor Modeling:  The Case of Adenosine A3Receptor Antagonists. An Approach to the Optimization of Protein Models
Tafi, Andrea / Bernardini, Cesare / Botta, Maurizio / Corelli, Federico / Andreini, Matteo / Martinelli, Adriano / Ortore, Gabriella / Baraldi, Pier Giovanni / Fruttarolo, Francesca / Borea, Pier Andrea et al. | 2006
4098
Design, Synthesis, and Structure−Activity Relationships of Novel 2-Substituted Pyrazinoylguanidine Epithelial Sodium Channel Blockers:  Drugs for Cystic Fibrosis and Chronic Bronchitis
Hirsh, Andrew J. / Molino, Bruce F. / Zhang, Jianzhong / Astakhova, Nadezhda / Geiss, William B. / Sargent, Bruce J. / Swenson, Brian D. / Usyatinsky, Alexander / Wyle, Michael J. / Boucher, Richard C. et al. | 2006
4116
Secondary Amides of Sulfonylated 3-Amidinophenylalanine. New Potent and Selective Inhibitors of Matriptase
Steinmetzer, Torsten / Schweinitz, Andrea / Stürzebecher, Anne / Dönnecke, Daniel / Uhland, Kerstin / Schuster, Oliver / Steinmetzer, Peter / Müller, Friedemann / Friedrich, Rainer / Than, Manuel E. et al. | 2006
4127
New 3-Alkylamino-4H-thieno-1,2,4-thiadiazine 1,1-Dioxide Derivatives Activate ATP-Sensitive Potassium Channels of Pancreatic Beta Cells
Nielsen, Flemming E. / Ebdrup, Søren / Jensen, Anette Frost / Ynddal, Lars / Bodvarsdottir, Thora B. / Stidsen, Carsten / Worsaae, Anne / Boonen, Harrie C. M. / Arkhammar, Per O. G. / Fremming, Tinna et al. | 2006
4140
Design, Synthesis, and Biological Evaluation of the Combinatorial Library with a New Spirodiketopiperazine Scaffold. Discovery of Novel Potent and Selective Low-Molecular-Weight CCR5 Antagonists
Habashita, Hiromu / Kokubo, Masaya / Hamano, Shin-ichi / Hamanaka, Nobuyuki / Toda, Masaaki / Shibayama, Shiro / Tada, Hideaki / Sagawa, Kenji / Fukushima, Daikichi / Maeda, Kenji et al. | 2006
4153
Is the σ2Receptor a Histone Binding Protein?
Colabufo, Nicola Antonio / Berardi, Francesco / Abate, Carmen / Contino, Marialessandra / Niso, Mauro / Perrone, Roberto | 2006
4153
Is the sigma~2 Receptor a Histone Binding Protein?
Colabufo, N. A. / Berardi, F. / Abate, C. / Contino, M. / Niso, M. / Perrone, R. | 2006
4159
2,5-Diketopiperazines as Potent, Selective, and Orally Bioavailable Oxytocin Antagonists. 3. Synthesis, Pharmacokinetics, and in Vivo Potency
Borthwick, Alan D. / Davies, Dave E. / Exall, Anne M. / Hatley, Richard J. D. / Hughes, Jennifer A. / Irving, Wendy R. / Livermore, David G. / Sollis, Steve L. / Nerozzi, Fabrizio / Valko, Klara L. et al. | 2006
4171
Iron Binding Dendrimers:  A Novel Approach for the Treatment of Haemochromatosis
Zhou, Tao / Neubert, Hendrik / Liu, Ding Yong / Liu, Zu Dong / Ma, Yong Min / Kong, Xiao Le / Luo, Wei / Mark, Sykes / Hider, Robert C. | 2006
4183
Acyclic Nucleoside Analogues as Inhibitors ofPlasmodiumfalciparumdUTPase
Nguyen, Corinne / Ruda, Gian Filippo / Schipani, Alessandro / Kasinathan, Ganasan / Leal, Isabel / Musso-Buendia, Alexander / Kaiser, Marcel / Brun, Reto / Ruiz-Pérez, Luis M. / Sahlberg, Britt-Louise et al. | 2006
4196
Activity of and Initial Mechanistic Studies on a Novel Antileishmanial Agent Identified through in Silico Pharmacophore Development and Database Searching
Delfín, Dawn A. / Bhattacharjee, Apurba K. / Yakovich, Adam J. / Werbovetz, Karl A. | 2006
4208
Back Door Modulation of the Farnesoid X Receptor:  Design, Synthesis, and Biological Evaluation of a Series of Side Chain Modified Chenodeoxycholic Acid Derivatives
Pellicciari, Roberto / Gioiello, Antimo / Costantino, Gabriele / Sadeghpour, Bahman M. / Rizzo, Giovanni / Meyer, Udo / Parks, Derek J. / Entrena-Guadix, Antonio / Fiorucci, Stefano | 2006
4216
Dissociated Nonsteroidal Glucocorticoid Receptor Modulators; Discovery of the Agonist Trigger in a Tetrahydronaphthalene−Benzoxazine Series
Barker, Mike / Clackers, Margaret / Copley, Royston / Demaine, Derek A. / Humphreys, Davina / Inglis, Graham G. A. / Johnston, Michael J. / Jones, Haydn T. / Haase, Michael V. / House, David et al. | 2006
4232
Virtual Screening of DNA Minor Groove Binders
Evans, David A. / Neidle, Stephen | 2006
4239
Further Structural Exploration of Trisubstituted Asymmetric Pyran Derivatives (2S,4R,5R)-2-Benzhydryl-5-benzylamino-tetrahydropyran-4-ol and Their Corresponding Disubstituted (3S,6S) Pyran Derivatives:  A Proposed Pharmacophore Model for High-Affinity Interaction with the Dopamine, Serotonin, and Norepinephrine Transporters
Zhang, Shijun / Fernandez, Fernando / Hazeldine, Stuart / Deschamps, Jeffrey / Zhen, Juan / Reith, Maarten E. A. / Dutta, Aloke K. | 2006
4248
From Ligand to Complexes: Inhibition of Human Immunodeficiency Virus Type 1 Integrase by b-Diketo Acid Metal Complexes
Sechi, M. / Bacchi, A. / Carcelli, M. / Compari, C. / Duce, E. / Fisicaro, E. / Rogolino, D. / Gates, P. / Derudas, M. / Al-Mawsawi, L.Q. et al. | 2006
4248
From Ligand to Complexes:  Inhibition of Human Immunodeficiency Virus Type 1 Integrase by β-Diketo Acid Metal Complexes
Sechi, Mario / Bacchi, Alessia / Carcelli, Mauro / Compari, Carlotta / Duce, Elenia / Fisicaro, Emilia / Rogolino, Dominga / Gates, Paul / Derudas, Marco / Al-Mawsawi, Laith Q. et al. | 2006
4248
From Ligand to Complexes: Inhibition of Human Immunodeficiency Virus Type 1 Integrase by beta-Diketo Acid Metal Complexes
Sechi, M. / Bacchi, A. / Carcelli, M. / Compari, C. / Duce, E. / Fisicaro, E. / Rogolino, D. / Gates, P. / Derudas, M. / Al-Mawsawi, L. Q. | 2006
4261
Docking and Three-Dimensional Quantitative Structure−Activity Relationship (3D QSAR) Analyses of Nonsteroidal Progesterone Receptor Ligands
Söderholm, Annu A. / Lehtovuori, Pekka T. / Nyrönen, Tommi H. | 2006
4269
C-(4,5,6-Trimethoxyindan-1-yl)methanamine:  A Mescaline Analogue Designed Using a Homology Model of the 5-HT2AReceptor
McLean, Thomas H. / Chambers, James J. / Parrish, Jason C. / Braden, Michael R. / Marona-Lewicka, Danuta / Kurrasch-Orbaugh, Deborah / Nichols, David E. | 2006
4275
Naphthyl and Coumarinyl Biarylpiperazine Derivatives as Highly Potent Human beta-Secretase Inhibitors. Design, Synthesis, and Enzymatic BACE-1 and Cell Assays
Garino, C. / Tomita, T. / Pietrancosta, N. / Laras, Y. / Rosas, R. / Herbette, G. / Maigret, B. / Quelever, G. / Iwatsubo, T. / Kraus, J.-L. | 2006
4275
Naphthyl and Coumarinyl Biarylpiperazine Derivatives as Highly Potent Human b-Secretase Inhibitors. Design, Synthesis, and Enzymatic BACE-1 and Cell Assays
Garino, C. / Tomita, T. / Pietrancosta, N. / Laras, Y. / Rosas, R. / Herbette, G. / Maigret, B. / Quelever, G. / Iwatsubo, T. / Kraus, J.-L. | 2006
4275
Naphthyl and Coumarinyl Biarylpiperazine Derivatives as Highly Potent Human β-Secretase Inhibitors. Design, Synthesis, and Enzymatic BACE-1 and Cell Assays
Garino, Cédrik / Tomita, Taisuke / Pietrancosta, Nicolas / Laras, Younes / Rosas, Roselyne / Herbette, Gaëtan / Maigret, Bernard / Quéléver, Gilles / Iwatsubo, Takeshi / Kraus, Jean-Louis | 2006
4286
Structural Requirements for the Substrates of the H+/Peptide Cotransporter PEPT2 Determined by Three-Dimensional Quantitative Structure−Activity Relationship Analysis
Biegel, Annegret / Gebauer, Sabine / Brandsch, Matthias / Neubert, Klaus / Thondorf, Iris | 2006
4297
Validation of a Novel CHX-A‘ ‘ Derivative Suitable for Peptide Conjugation:  Small Animal PET/CT Imaging Using Yttrium-86-CHX-A‘ ‘-Octreotide
Clifford, Thomas / Boswell, C. Andrew / Biddlecombe, Gráinne B. / Lewis, Jason S. / Brechbiel, Martin W. | 2006
4305
Proposal of a New Binding Orientation for Non-Peptide AT1 Antagonists:  Homology Modeling, Docking and Three-Dimensional Quantitative Structure−Activity Relationship Analysis
Tuccinardi, Tiziano / Calderone, Vincenzo / Rapposelli, Simona / Martinelli, Adriano | 2006
4317
New Furan Side Tetracyclic Allopsoralen Derivatives:  Synthesis and Photobiological Evaluation
Dalla Via, Lisa / Mammi, Stefano / Uriarte, Eugenio / Santana, Lourdes / Lampronti, Ilaria / Gambari, Roberto / Gia, Ornella | 2006
4327
Design and Synthesis of Novel 2-Amino-5-hydroxyindole Derivatives That Inhibit Human 5-Lipoxygenase
Landwehr, Jens / George, Sven / Karg, Eva-Maria / Poeckel, Daniel / Steinhilber, Dieter / Troschuetz, Reinhard / Werz, Oliver | 2006
4333
Design, Synthesis, and Biological Evaluation of Cyclic and Acyclic Nitrobenzylphosphoramide Mustards forE.coliNitroreductase Activation
Jiang, Yongying / Han, Jiye / Yu, Chengzhi / Vass, Simon O. / Searle, Peter F. / Browne, Patrick / Knox, Richard J. / Hu, Longqin | 2006
4344
Kinetics and Mechanisms of Activation of a-Amino Acid Ester Prodrugs of Camptothecins
Song, L. / Bevins, R. / Anderson, B.D. | 2006
4344
Kinetics and Mechanisms of Activation of α-Amino Acid Ester Prodrugs of Camptothecins
Song, Lin / Bevins, Robert / Anderson, Bradley D. | 2006
4344
Kinetics and Mechanisms of Activation of alpha-Amino Acid Ester Prodrugs of Camptothecins
Song, L. / Bevins, R. / Anderson, B. D. | 2006
4356
Antitumor Activity of JS-K [O2-(2,4-Dinitrophenyl) 1-[(4-Ethoxycarbonyl)piperazin-1-yl]diazen-1-ium-1,2-diolate] and RelatedO2-Aryl Diazeniumdiolates in Vitro and in Vivo
Shami, Paul J. / Saavedra, Joseph E. / Bonifant, Challice L. / Chu, Jingxi / Udupi, Vidya / Malaviya, Swati / Carr, Brian I. / Kar, Siddhartha / Wang, Meifeng / Jia, Lee et al. | 2006
4367
Line-Walking Method for Predicting the Inhibition of P450 Drug Metabolism
Hudelson, Matthew G. / Jones, Jeffrey P. | 2006
4374
(R)-3‘-(3-Methylbenzo[b]thiophen-5-yl)spiro[1-azabicyclo[2,2,2]octane-3,5‘-oxazolidin]-2‘-one, a Novel and Potent α7 Nicotinic Acetylcholine Receptor Partial Agonist Displays Cognitive Enhancing Properties
Tatsumi, Ryo / Fujio, Masakazu / Takanashi, Shin-ichi / Numata, Atsushi / Katayama, Jiro / Satoh, Hiroyuki / Shiigi, Yasuyuki / Maeda, Jun-ichi / Kuriyama, Makoto / Horikawa, Takashi et al. | 2006
4374
(R)-3'-(3-Methylbenzo[b]thiophen-5-yl)spiro[1-azabicyclo-[2,2,2]octane-3,5'-oxazolidin]-2'-one, a Novel and Potent alpha7 Nicotinic Acetylcholine Receptor Partial Agonist Displays Cognitive Enhancing Properties
Tatsumi, R. / Fujio, M. / Takanashi, S.-i. / Numata, A. / Katayama, J. / Satoh, H. / Shiigi, Y. / Maeda, J.-i. / Kuriyama, M. / Horikawa, T. | 2006
4374
(R)-3'-(3-Methylbenzo[b]thiophen-5-yl)spiro[1-azabi- cyclo[2,2,2]octane-3,5'-oxazolidin]-2'-one, a Novel and Potent a7 Nicotinic Acetylcholine Receptor Partial Agonist Displays Cognitive Enhancing Properties
Tatsumi, R. / Fujio, M. / Takanashi, S.-i. / Numata, A. / Katayama, J. / Satoh, H. / Shiigi, Y. / Maeda, J.-i. / Kuriyama, M. / Horikawa, T. et al. | 2006
4384
A New Synthesis of Sulfonamides by Aminolysis ofp-Nitrophenylsulfonates Yielding Potent and Selective Adenosine A2BReceptor Antagonists
Yan, Luo / Bertarelli, Daniela C. G. / Hayallah, Alaa M. / Meyer, Heiko / Klotz, Karl-Norbert / Müller, Christa E. | 2006
4392
Semisynthetic Maytansine Analogues for the Targeted Treatment of Cancer
Widdison, Wayne C. / Wilhelm, Sharon D. / Cavanagh, Emily E. / Whiteman, Kathleen R. / Leece, Barbara A. / Kovtun, Yelena / Goldmacher, Victor S. / Xie, Hongsheng / Steeves, Rita M. / Lutz, Robert J. et al. | 2006
4409
Novel Selective Inhibitors of Neutral Endopeptidase for the Treatment of Female Sexual Arousal Disorder. Synthesis and Activity of Functionalized Glutaramides
Pryde, David C. / Maw, Graham N. / Planken, Simon / Platts, Michelle Y. / Sanderson, Vivienne / Corless, Martin / Stobie, Alan / Barber, Christopher G. / Russell, Rachel / Foster, Laura et al. | 2006
4425
Discovery ofN-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an Agonist of the α7 Nicotinic Acetylcholine Receptor, for the Potential Treatment of Cognitive Deficits in Schizophrenia:  Synthesis and Structure−Activity Relationship
Wishka, Donn G. / Walker, Daniel P. / Yates, Karen M. / Reitz, Steven C. / Jia, Shaojuan / Myers, Jason K. / Olson, Kirk L. / Jacobsen, E. Jon / Wolfe, Mark L. / Groppi, Vincent E. et al. | 2006
4425
Discovery of N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]furo[2,3-c&- #93;pyridine-5-carboxamide, an Agonist of the a7 Nicotinic Acetylcholine Receptor, for the Potential Treatment of Cognitive Deficits in Schizophrenia: Synthesis and Structure-Activity Relationship
Wishka, D.G. / Walker, D.P. / Yates, K.M. / Reitz, S.C. / Jia, S. / Myers, J.K. / Olson, K.L. / Jacobsen, E.J. / Wolfe, M.L. / Groppi, V.E. et al. | 2006
4425
Discovery of N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an Agonist of the alpha7 Nicotinic Acetylcholine Receptor, for the Potential Treatment of Cognitive Deficits in Schizophrenia: Synthesis and Structure-Activity Relationship
Wishka, D. G. / Walker, D. P. / Yates, K. M. / Reitz, S. C. / Jia, S. / Myers, J. K. / Olson, K. L. / Jacobsen, E. J. / Wolfe, M. L. / Groppi, V. E. | 2006
4437
Imidazole−Dioxolane Compounds as Isozyme-Selective Heme Oxygenase Inhibitors
Vlahakis, Jason Z. / Kinobe, Robert T. / Bowers, Raymond J. / Brien, James F. / Nakatsu, Kanji / Szarek, Walter A. | 2006
4442
Hydroxy-1,2,5-oxadiazolyl Moiety as Bioisoster of the Carboxy Function. Synthesis, Ionization Constants, and Pharmacological Characterization of gamma-Aminobutyric Acid (GABA) Related Compounds
Lolli, M. L. / Hansen, S. L. / Rolando, B. / Nielsen, B. / Wellendorph, P. / Madsen, K. / Larsen, O. M. / Kristiansen, U. / Fruttero, R. / Gasco, A. | 2006
4442
Hydroxy-1,2,5-oxadiazolyl Moiety as Bioisoster of the Carboxy Function. Synthesis, Ionization Constants, and Pharmacological Characterization of γ-Aminobutyric Acid (GABA) Related Compounds
Lolli, Marco L. / Hansen, Suzanne L. / Rolando, Barbara / Nielsen, Birgitte / Wellendorph, Petrine / Madsen, Karsten / Larsen, Orla Miller / Kristiansen, Uffe / Fruttero, Roberta / Gasco, Alberto et al. | 2006