- Discovery of Novel CB2 Receptor Ligands by a Pharmacophore-Based Virtual Screening Workflow.
[作者：Markt, Patrick;Feldmann, Clemens;Rollinger, Judith Maria;Raduner, Stefan;Schuster, Daniela;Kirchmair, Johannes;Distinto, Simona;Spitzer, Gudrun Maria;Wolber, Gerhard;Laggner, Christian;Altmann, Karl-Heinz;Langer, Thierry;Gertsch, Jurg;,期刊：Journal of Medicinal Chemistry, 页码：369-378 , 文章类型： 研究论文，,卷期：2009年52-2]
- Cannabinoid receptor 2 (CB2 receptor) ligands are potential candidates for the therapy of chronic pain, inflammatory disorders, atherosclerosis, and osteoporosis. We describe the development of pharmacophore models for ...
- Edaravone Derivatives Containing NO-Donor Functions.
[作者：Chegaev, Konstantin;Cena, Clara;Giorgis, Marta;Rolando, Barbara;Tosco, Paolo;Bertinaria, Massimo;Fruttero, Roberta;Carrupt, Pierre-Alain;Gasco, Alberto;,期刊：Journal of Medicinal Chemistry, 页码：574-578 , 文章类型： 研究论文，,卷期：2009年52-2]
- A new series of polyvalent drugs obtained by joining edaravone with NO-donor moieties is described. All compds. display high antioxidant power together with NO-dependent vasodilator properties. The anal. of a no. of mo...
- Fragment-Based Discovery of the Pyrazol-4-yl Urea (AT9283), a Multitargeted Kinase Inhibitor with Potent Aurora Kinase Activity.
[作者：Howard, Steven;Berdini, Valerio;Boulstridge, John A.;Carr, Maria G.;Cross, David M.;Curry, Jayne;Devine, Lindsay A.;Early, Theresa R.;Fazal, Lynsey;Gill, Adrian L.;Heathcote, Michelle;Maman, Sarita;Matthews, Julia E.;McMenamin, Rachel L.;Navarro, Eva F.;O,期刊：Journal of Medicinal Chemistry, 页码：379-388 , 文章类型： 研究论文，,卷期：2009年52-2]
- Here, we describe the identification of a clin. candidate via structure-based optimization of a ligand efficient pyrazole-benzimidazole fragment. Aurora kinases play a key role in the regulation of mitosis and in recent...
- Induced Association of m Opioid (MOP) and Type 2 Cholecystokinin (CCK2) Receptors by Novel Bivalent Ligands.
[作者：Zheng, Yaguo;Akgun, Eyup;Harikumar, Kaleeckal G.;Hopson, Jessika;Powers, Michael D.;Lunzer, Mary M.;Miller, Laurence J.;Portoghese, Philip S.;,期刊：Journal of Medicinal Chemistry, 页码：247-258 , 文章类型： 研究论文，,卷期：2009年52-2]
- Both m-opioid (MOP) and type 2 cholecystokinin (CCK2) receptors are present in areas of the central nervous system that are involved in modulation of pain processing. We conducted bioluminescence resonance energy transf...
- A series of halogenated heterodimeric inhibitors of prostate specific membrane antigen (PSMA) as radiolabeled probes for targeting prostate cancer.
[作者：Maresca, K. P.;Hillier, S. M.;Femia, F. J.;Keith, D.;Barone, C.;Joyal, J. L.;Zimmerman, C. N.;Kozikowski, A. P.;Barrett, J. A.;Eckelman, W. C.;Babich, J. W.;,期刊：Journal of Medicinal Chemistry, 页码：347-357 , 文章类型： 研究论文，,卷期：2009年52-2]
- Prostate specific membrane antigen (PSMA) is a validated mol. marker for prostate cancer. A series of glutamate-urea (Glu-urea-X) heterodimeric inhibitors of PSMA were designed and synthesized where X = e-N-(o-I, m-I, p...
- Discovery of Human Macrophage Migration Inhibitory Factor (MIF)-CD74 Antagonists via Virtual Screening.
[作者：Cournia, Zoe;Leng, Lin;Gandavadi, Sunilkumar;Du, Xin;Bucala, Richard;Jorgensen, William L.;,期刊：Journal of Medicinal Chemistry, 页码：416-424 , 文章类型： 研究论文，,卷期：2009年52-2]
- Macrophage migration inhibitory factor (MIF) is a cytokine that is involved in the regulation of inflammation as well as cell proliferation and differentiation. Deactivation of MIF by antibodies or inhibition of MIF bin...
- Combining 4-Aminoquinoline- and Clotrimazole-Based Pharmacophores toward Innovative and Potent Hybrid Antimalarials.
[作者：Gemma, Sandra;Campiani, Giuseppe;Butini, Stefania;Joshi, Bhupendra P.;Kukreja, Gagan;Coccone, Salvatore Sanna;Bernetti, Matteo;Persico, Marco;Nacci, Vito;Fiorini, Isabella;Novellino, Ettore;Taramelli, Donatella;Basilico, Nicoletta;Parapini, Silvia;Yardley,期刊：Journal of Medicinal Chemistry, 页码：502-513 , 文章类型： 研究论文，,卷期：2009年52-2]
- Antimalarial agents structurally based on novel pharmacophores, synthesized by low-cost synthetic procedures and characterized by low potential for developing resistance are urgently needed. Recently, we developed an in...
- Oligodeoxyribonucleotide-Based Antagonists for Toll-Like Receptors 7 and 9.
[作者：Wang, Daqing;Bhagat, Lakshmi;Yu, Dong;Zhu, Fu-Gang;Tang, Jimmy X.;Kandimalla, Ekambar R.;Agrawal, Sudhir;,期刊：Journal of Medicinal Chemistry, 页码：551-558 , 文章类型： 研究论文，,卷期：2009年52-2]
- Oligodeoxyribonucleotides contg. unmethylated CpG motifs act as TLR9 agonists. In this study, we evaluated oligonucleotides contg. an unmethylated CpG motif in which two nucleotides adjacent to the CpG dinucleotide were...
- Pt(II) Complexes of a Combretastatin A-4 Analogous Chalcone: Effects of Conjugation on Cytotoxicity, Tumor Specificity, and Long-Term Tumor Growth Suppression.
[作者：Schobert, Rainer;Biersack, Bernhard;Dietrich, Andrea;Knauer, Sebastian;Zoldakova, Miroslava;Fruehauf, Angelika;Mueller, Thomas;,期刊：Journal of Medicinal Chemistry, 页码：241-246 , 文章类型： 研究论文，,卷期：2009年52-2]
- Three dichlorido(6-aminomethylnicotinate)platinum complexes 6 comprising a combretastatin A-4 analogous chalcone were tested on a panel of 21 tumor cell lines from 9 entities. Parent chalcone 1a and the directly linked ...
- Total Synthesis and Biological Evaluation of Tubulysin U, Tubulysin V, and Their Analogues.
[作者：Balasubramanian, Ranganathan;Raghavan, Bhooma;Begaye, Adrian;Sackett, Dan L.;Fecik, Robert A.;,期刊：Journal of Medicinal Chemistry, 页码：238-240 , 文章类型： 研究论文，,卷期：2009年52-2]
- A stereoselective total synthesis of the cytotoxic natural products tubulysin U, tubulysin V, and its unnatural epimer epi-tubulysin V, is reported. Simplified analogs contg. N,N-dimethyl-D-alanine as a replacement for ...
- Berberine Analogues as a Novel Class of the Low-Density-Lipoprotein Receptor Up-Regulators: Synthesis, Structure-Activity Relationships, and Cholesterol-Lowering Efficacy.
[作者：Li, Ying-Hong;Yang, Peng;Kong, Wei-Jia;Wang, Yan-Xiang;Hu, Chang-Qin;Zuo, Zeng-Yan;Wang, Yue-Ming;Gao, Hong;Gao, Li-Mei;Feng, Yan-Chun;Du, Na-Na;Liu, Ying;Song, Dan-Qing;Jiang, Jian-Dong;,期刊：Journal of Medicinal Chemistry, 页码：492-501 , 文章类型： 研究论文，,卷期：2009年52-2]
- Twenty-nine derivs. of berberine I (R1 = MeO, R2 = H) (II) or pseudoberberine I (R1 = H, R2 = MeO) (III) were designed, semisynthesized, and evaluated for their up-regulatory activity on the low-d.-lipoprotein receptor (...
- Discovery of the Poly(ADP-ribose) Polymerase (PARP) Inhibitor 2-[(R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide (ABT-888) for the Treatment of Cancer.
[作者：Penning, Thomas D.;Zhu, Gui-Dong;Gandhi, Viraj B.;Gong, Jianchun;Liu, Xuesong;Shi, Yan;Klinghofer, Vered;Johnson, Eric F.;Donawho, Cherrie K.;Frost, David J.;Bontcheva-Diaz, Velitchka;Bouska, Jennifer J.;Osterling, Donald J.;Olson, Amanda M.;Marsh, Kennan,期刊：Journal of Medicinal Chemistry, 页码：514-523 , 文章类型： 研究论文，,卷期：2009年52-2]
- A series of cyclic amine-contg. benzimidazole carboxamide PARP inhibitors with a methyl-substituted quaternary center at the point of attachment to the benzimidazole ring system has been developed. These compds. exhibit ...
- 6-Methoxy-N-alkyl Isatin Acylhydrazone Derivatives as a Novel Series of Potent Selective Cannabinoid Receptor 2 Inverse Agonists: Design, Synthesis, and Binding Mode Prediction.
[作者：Diaz, Philippe;Phatak, Sharangdhar S.;Xu, Jijun;Astruc-Diaz, Fanny;Cavasotto, Claudio N.;Naguib, Mohamed;,期刊：Journal of Medicinal Chemistry, 页码：433-444 , 文章类型： 研究论文，,卷期：2009年52-2]
- Recently, we discovered and reported a series of N-alkyl isatin acylhydrazone derivs. that are potent CB2 agonists. Here, we describe a novel series of selective CB2 inverse agonists resulting from introduction of a met...
- Docking Studies on a New Human Immunodeficiency Virus Integrase-Mg-DNA Complex: Phenyl Ring Exploration and Synthesis of 1H-Benzylindole Derivatives through Fluorine Substitutions.
[作者：Ferro, Stefania;De Luca, Laura;Barreca, Maria Letizia;Iraci, Nunzio;De Grazia, Sara;Christ, Frauke;Witvrouw, Myriam;Debyser, Zeger;Chimirri, Alba;,期刊：Journal of Medicinal Chemistry, 页码：569-573 , 文章类型： 研究论文，,卷期：2009年52-2]
- A new model of HIV-1 integrase-Mg-DNA complex that is useful for docking expts. has been built. It was used to study the binding mode of integrase strand transfer inhibitor I (CHI-1043) and other fluorine analogs. Mol....
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