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文章名     作者     期刊名     摘要     卷     期         如果没有找到您所需要的文献，请点击 ——此处申请     共19条记录   Electron Paramagnetic Resonance (EPR) Study of Spin-Labeled Camptothecin Derivatives: A Different Look of the Ternary Complex [作者：RICCI ANTONIO; MARINELLO JESSICA; BORTOLUS MARCO; SANCHEZ ALBERT; GRANDAS ANNA; PEDROSO ENRIQUE; POMMIER YVES; CAPRANICO GIOVANNI; MANIERO ANNA LISA; ZAGOTTO GIUSEPPE,期刊：Journal of Medicinal Chemistry, 页码：1003-1009 , 文章类型： Article，,卷期：2011年54-4] Camptothecin (CPT) derivatives are clinically effective poisons of DNA topoisomerase I (Top 1) able to form a ternary complex with the Top1 DNA complex. The aim of this investigation was to examine the dynamic aspects of... 2-Aminothiazoles as Therapeutic Leads for Prion Diseases [作者：GALLARDOGODOY ALEJANDRA; GEVER JOEL; FIFE KIMBERLY L; SILBER B MICHAEL; PRUSINER STANLEY B; RENSLO ADAM R,期刊：Journal of Medicinal Chemistry, 页码：1010-1021 , 文章类型： Article，,卷期：2011年54-4] 2-Aminothiazoles are a new class of small molecules with antiprion activity in prion-infected neuroblastoma cell lines (J. Virol. 2010, 84, 3408). We report here structure-activity studies undertaken to improve the poten... Analogues of sigma Receptor Ligand 1-Cyclohexyl-4[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]pip erazine (PB28) with Added Polar Functionality and Reduced Lipophilicity for Potential Use as Positron Emission Tomography Radiotracers [作者：ABATE CARMEN; NISO MAURO; LACIVITA ENZA; MOSIER PHILIP D; TOSCANO ANNAMARIA; PERRONE ROBERTO,期刊：Journal of Medicinal Chemistry, 页码：1022-1032 , 文章类型： Article，,卷期：2011年54-4] 1-Cyclohexyl-4[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]pip erazine 1 (PB28) represents an excellent lead candidate for therapeutic and/or diagnostic applications in oncology. However, because its utility is... Evaluation of Quinazoline Analogues as Glucocerebrosidase Inhibitors with Chaperone Activity [作者：MARUGAN JUAN J; ZHENG WEI; MOTABAR OMID; SOUTHALL NOEL; GOLDIN EHUD; WESTBROEK WENDY; STUBBLEFIELD BARBARA K; SIDRANSKY ELLEN; AUNGST RONALD A; LEA WENDY A; SIMEONOV ANTON; LEISTER WILLIAM; AUSTIN CHRISTOPHER P,期刊：Journal of Medicinal Chemistry, 页码：1033-1058 , 文章类型： Article，,卷期：2011年54-4] Gaucher disease is a lysosomal storage disorder (LSD) caused by deficiency in the enzyme glucocerebrosidase (GC). Small molecule chaperones of protein folding and translocation have been proposed as a promising therapeut... Acyloxy Nitroso Compounds as Nitroxyl (HNO) Donors: Kinetics, Reactions with Thiols, and Vasodilation Properties [作者：SHOMAN MAI E; DUMOND JENNA F; ISBELL T S; CRAWFORD J H; BRANDON ANGELA; HONOVAR JAIDEEP; VITTURI DARIO A; WHITE C R; PATEL R P; KING S BRUCE,期刊：Journal of Medicinal Chemistry, 页码：1059-1070 , 文章类型： Article，,卷期：2011年54-4] Acyloxy nitroso compounds hydrolyze to nitroxyl (HNO), a nitrogen monoxide with distinct chemistry and biology. Ultraviolet-visible spectroscopy and mass spectrometry show hydrolysis rate depends on pH and ester group st... Discovery and Biological Characterization of (2R,4S)-1 '-Acetyl-N-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl}-2-(4-fluoro-2- methylphenyl)-N-methyl-4,4 '-bipiperidine-1-carboxamide as a New Potent and Selective Neurokinin 1 (NK1) Receptor Antagonist Clinical Candidate [作者：DI FABIO ROMANO; ALVARO GIUSEPPE; GRIFFANTE CRISTIANA; PIZZI DOMENICA A; DONATI DANIELE; MATTIOLI MARIO; CIMAROSTI ZADEO; GUERCIO GIUSEPPE; MARCHIORO CARLA; PROVERA STEFANO; ZONZINI LAURA; MONTANARI DINO; MELOTTO SERGIO; GERRARD PHILIP A; TRIST DAVID G; RATTI EMILIANGELO; CORSI MAURO,期刊：Journal of Medicinal Chemistry, 页码：1071-1079 , 文章类型： Article，,卷期：2011年54-4] A large body of compelling preclinical evidence supports the clinical use of neurokinin (NK) receptor antagonists in a plethora of CNS and non-CNS therapeutic areas. The significant investment made in this area over the ... Biotin Ergopeptide Probes for Dopamine Receptors [作者：VENDRELL MARC; MOLERO ANABEL; GONZALEZ SERGIO; PEREZCAPOTE KAMIL; LLUIS CARME; MCCORMICK PETER J; FRANCO RAFAEL; CORTES ANTONI; CASADO VICENT; ALBERICIO FERNANDO; ROYO MIRIAM,期刊：Journal of Medicinal Chemistry, 页码：1080-1090 , 文章类型： Article，,卷期：2011年54-4] The incorporation of chemical modifications into the structure of bioactive compounds is often difficult because the biological properties of the new molecules must be retained with respect to the native ligand. Ergopept... Convergent Evolution-Guided Design of Antimicrobial Peptides Derived from Influenza A Virus Hemagglutinin [作者：ZHU SHUNYI; AUMELAS ANDRE; GAO BIN,期刊：Journal of Medicinal Chemistry, 页码：1091-1095 , 文章类型： Article，,卷期：2011年54-4] Antimicrobial activity and solution structures of four 13-amino acid peptides derived from the fusion domain of viral hemagglutinin proteins are presented. The results show that carboxyl-terminal amidation is a key facto... Development of Non-Peptide Ligands of Growth Factor Receptor-Bound Protein 2-Src Homology 2 Domain Using Molecular Modeling and NMR Spectroscopy [作者：ORCAJORINCON ANGEL L; ORTEGAGUTIERREZ SILVIA; SERRANO PEDRO; TORRECILLAS IVAN R; WUETHRICH KURT; CAMPILLO MERCEDES; PARDO LEONARDO; VISO ALMA; BENHAMU BELLINDA; LOPEZRODRIGUEZ MARIA L,期刊：Journal of Medicinal Chemistry, 页码：1096-1100 , 文章类型： Article，,卷期：2011年54-4] We report a novel series of non-peptide ligands that inhibit the growth factor receptor-bound protein 2 (Grb2)-Src homology 2 (SH2) domain binding, designed using a combined computational and NMR-driven approach. We have... 3-Thiomorpholin-8-oxo-8H-acenaphtho[1,2-b]pyrrole-9-carbonitrile (S1) Based Molecules as Potent, Dual Inhibitors of B-Cell Lymphoma 2 (Bcl-2) and Myeloid Cell Leukemia Sequence 1 (Mcl-1): Structure-Based Design and Structure-Activity Relationship Studies [作者：ZHANG ZHICHAO; WU GUIYE; XIE FEIBO; SONG TING; CHANG XILONG,期刊：Journal of Medicinal Chemistry, 页码：1101-1105 , 文章类型： Article，,卷期：2011年54-4] We recently described the discovery of a dual inhibitor of Bcl-2 and Mcl-1, 3-thiomorpholin-8-oxo-8H-acenaphtho[1,2-b]pyrrole-9-carbonitrile (3, S1). Here we report a structure-guided design in combination with structure... Discovery, Synthesis, and Structure-Activity Relationship Development of a Series of N-(4-Acetamido)phenylpicolinamides as Positive Allosteric Modulators of Metabotropic Glutamate Receptor 4 (mGlu(4)) with CNS Exposure in Rats [作者：ENGERS DARREN W; FIELD JULIE R; LE UYEN; ZHOU YA; BOLINGER JULIE D; ZAMORANO ROCIO; BLOBAUM ANNA L; JONES CARRIE K; JADHAV SATYAWAN; WEAVER C DAVID; CONN P JEFFREY; LINDSLEY CRAIG W; NISWENDER COLLEEN M; HOPKINS COREY R,期刊：Journal of Medicinal Chemistry, 页码：1106-1110 , 文章类型： Article，,卷期：2011年54-4] Herein we report the discovery, synthesis, and evaluation of a series of N-(4-acetamido)-phenylpico-linamides as positive allosteric modulators of mGlu(4). Compounds from the series show submicromolar potency at both hum... ATP-Binding Site of Bacterial Enzymes as a Target for Antibacterial Drug Design [作者：SKEDELJ VERONIKA; TOMASIC TIHOMIR; MASIC LUCIJA PETERLIN; ZEGA ANAMARIJA,期刊：Journal of Medicinal Chemistry, 页码：915-929 , 文章类型： Article，,卷期：2011年54-4] X-ray Crystal Structure and Binding Mode Analysis of Human S-Adenosylhomocysteine Hydrolase Complexed with Novel Mechanism-Based Inhibitors, Haloneplanocin A Analogues [作者：LEE KANG MAN; CHOI WON JUN; LEE YOONJI; LEE HYUN JOO; ZHAO LONG XUAN; LEE HYUK WOO; PARK JAE GYU; KIM HEA OK; HWANG KWANG YEON; HEO YONGSEOK; CHOI SUN; JEONG LAK SHIN,期刊：Journal of Medicinal Chemistry, 页码：930-938 , 文章类型： Article，,卷期：2011年54-4] The X-ray crystal structure of human S-adenosylhomocysteine (AdoHcy) hydrolase was first determined as a tetrameric form bound with the novel mechanism-based inhibitor fluoroneplanocin A (4b). The crystallized enzyme com... Development and Evaluation of Endothelin-A Receptor (Radio)Ligands for Positron Emission Tomography [作者：MICHEL KRISTIN; BUETHER KATRIN; LAW MARILYN P; WAGNER STEFAN; SCHOBER OTMAR; HERMANN SVEN; SCHAEFERS MICHAEL; RIEMANN BURKHARD; HOELTKE CARSTEN; KOPKA KLAUS,期刊：Journal of Medicinal Chemistry, 页码：939-948 , 文章类型： Article，,卷期：2011年54-4] The expression and function of endothelin (ET) receptors are abnormal in cardiovascular diseases, tumor progression, and tumor metastasis. A previously reported promising radioligand for positron emission tomography (PET... Synthesis and Evaluation of C-11-Labeled Imidazo[2,1-b]benzothiazoles (IBTs) as PET Tracers for Imaging beta-Amyloid Plaques in Alzheimer's Disease [作者：YOUSEFI BEHROOZ H; MANOOK ANDRE; DRZEZGA ALEXANDER; REUTERN BORIS V; SCHWAIGER MARKUS; WESTER HANSJUERGEN; HENRIKSEN GJERMUND,期刊：Journal of Medicinal Chemistry, 页码：949-956 , 文章类型： Article，,卷期：2011年54-4] We report a novel series of C-11-labeled imidazo[2,1-b]benzothiazoles (IBTs) as tracers for imaging of cerebral beta-amyloid (A beta) deposits in patients with Alzheimer's disease (AD) by means of positron emission tomog... Probes for Narcotic Receptor Mediated Phenomena. 41. Unusual Inverse mu-Agonists and Potent mu-Opioid Antagonists by Modification of the N-Substituent in Enantiomeric 5-(3-Hydroxyphenyl)morphans [作者：CHENG KEJUN; LEE YONG SOK; ROTHMAN RICHARD B; DERSCH CHRISTINA M; BITTMAN ROSS W; JACOBSON ARTHUR E; RICE KENNER C,期刊：Journal of Medicinal Chemistry, 页码：957-969 , 文章类型： Article，,卷期：2011年54-4] Conformational restraint in the N-substituent of enantiomeric 5-(3-hydroxyphenyl)morphans was conferred by the addition of a cyclopropane ring or a double bond. All of the possible enantiomers and isomers of the N-substi...