- Structural Evolutions of Salicylaldoximes as Selective Agonists for Estrogen Receptor b.
[作者：Minutolo, Filippo;Bertini, Simone;Granchi, Carlotta;Marchitiello, Teresa;Prota, Giovanni;Rapposelli, Simona;Tuccinardi, Tiziano;Martinelli, Adriano;Gunther, Jillian R.;Carlson, Kathryn E.;Katzenellenbogen, John A.;Macchia, Marco;,期刊：Journal of Medicinal Chemistry, 页码：858-867 , 文章类型： 研究论文，,卷期：2009年52-3]
- The bioisosteric replacement of the phenol ring, a signature functional group of most estrogen receptor (ER) ligands, with a hydrogen-bonded pseudocyclic ring, led to the development of a novel class of non-steroidal ER-...
- Therapeutic Index of Gramicidin S is Strongly Modulated by D-Phenylalanine Analogues at the b-Turn.
[作者：Solanas, Concepcion;de la Torre, Beatriz G.;Fernandez-Reyes, Maria;Santiveri, Clara M.;Jimenez, M. Angeles;Rivas, Luis;Jimenez, Ana I.;Andreu, David;Cativiela, Carlos;,期刊：Journal of Medicinal Chemistry, 页码：664-674 , 文章类型： 研究论文，,卷期：2009年52-3]
- Analogs of the cationic antimicrobial peptide gramicidin S (GS), cyclo(Val-Orn-Leu-D-Phe-Pro)2, with D-Phe residues replaced by different (restricted mobility, mostly) surrogates have been synthesized and used in SAR stu...
- Discovery of Highly Potent and Selective Inhibitors of Neuronal Nitric Oxide Synthase by Fragment Hopping.
[作者：Ji, Haitao;Li, Huiying;Martasek, Pavel;Roman, Linda J.;Poulos, Thomas L.;Silverman, Richard B.;,期刊：Journal of Medicinal Chemistry, 页码：779-797 , 文章类型： 研究论文，,卷期：2009年52-3]
- Selective inhibition of neuronal nitric oxide synthase (nNOS) has been shown to prevent brain injury and is important for the treatment of various neurodegenerative disorders. This study shows that not only greater inhi...
- Structure and Activity of (2,8)-Dicarba-(3,12)-cystino a-ImI, an a-Conotoxin Containing a Nonreducible Cystine Analogue.
[作者：MacRaild, Christopher A.;Illesinghe, Jayamini;van Lierop, Bianca J.;Townsend, Amanda L.;Chebib, Mary;Livett, Bruce G.;Robinson, Andrea J.;Norton, Raymond S.;,期刊：Journal of Medicinal Chemistry, 页码：755-762 , 文章类型： 研究论文，,卷期：2009年52-3]
- The a-conotoxins are potent and selective antagonists of nicotinic acetylcholine receptors (nAChR). Exploitation of these and other peptides in research and clin. settings has been hampered by the lability of the disulf...
- Targeting the delivery of glycan-based paclitaxel prodrugs to cancer cells via glucose transporters.
[作者：Lin, Yih-Shyan;Tungpradit, Rudeewan;Sinchaikul, Supachok;An, Feng-Ming;Liu, Der-Zen;Phutrakul, Suree;Chen, Shui-Tein;,期刊：Journal of Medicinal Chemistry, 页码：889-889 , 文章类型： 研究论文，,卷期：2009年52-3]
- On page 7428, an addnl. corresponding author as Der-Zen Liu wasn't denoted with an asterisk in the Author line. On page 7428, in the Address line, the final address should read: "Graduate Institute of Biomedical materia...
- Design, Synthesis, and Evaluation of Potent, Nonpeptidic Mimetics of Second Mitochondria-Derived Activator of Caspases.
[作者：Sun, Wei;Nikolovska-Coleska, Zaneta;Qin, Dongguang;Sun, Haiying;Yang, Chao-Yie;Bai, Longchuang;Qiu, Su;Wang, You;Ma, Dawei;Wang, Shaomeng;,期刊：Journal of Medicinal Chemistry, 页码：593-596 , 文章类型： 研究论文，,卷期：2009年52-3]
- A series of new Smac mimetics have been designed, synthesized, and evaluated. The most potent compd. 10 (I) binds to XIAP, cIAP-1, and cIAP-2 BIR3 proteins with Ki of 3.9, 0.37, and 0.25 nM, resp. Compd. 10 antagonizes...
- Pyrazolo[1,5-a]-1,3,5-triazine as a Purine Bioisostere: Access to Potent Cyclin-Dependent Kinase Inhibitor (R)-Roscovitine Analogue.
[作者：Popowycz, Florence;Fournet, Guy;Schneider, Cedric;Bettayeb, Karima;Ferandin, Yoan;Lamigeon, Cyrile;Tirado, Oscar M.;Mateo-Lozano, Silvia;Notario, Vicente;Colas, Pierre;Bernard, Philippe;Meijer, Laurent;Joseph, Benoit;,期刊：Journal of Medicinal Chemistry, 页码：655-663 , 文章类型： 研究论文，,卷期：2009年52-3]
- Pharmacol. inhibitors of cyclin-dependent kinases (CDKs) have a wide therapeutic potential. Among the CDK inhibitors currently under clin. trials, the 2,6,9-trisubstituted purine (R)-roscovitine displays rather high sel...
- Synthesis of Novel 4,6-Di(substituted)amino-1,2-dihydro-1,3,5-triazine Derivatives as Topical Antiseptic Agents.
[作者：Maeda, Shirou;Kita, Toshiko;Meguro, Kanji;,期刊：Journal of Medicinal Chemistry, 页码：597-600 , 文章类型： 研究论文，,卷期：2009年52-3]
- A series of novel 4,6-di(substituted)amino-1,2-dihydro-1,3,5-triazines I (R1 = Ph, PhCH2CH2, n-octyl, 4-MeOC6H4CH2, etc.; R2 = Et, n-Pr, n-Bu, n-octyl, n-decyl, etc.), designed to have ClogP of 5.1-7.5, was synthesized a...
- Design, synthesis, and cytoprotective effect of 2-aminothiazole analogues as potent poly(ADP-ribose) polymerase-1 Inhibitors.
[作者：Zhang, Wen-Ting;Ruan, Jin-Lan;Wu, Peng-Fei;Jiang, Feng-Chao;Zhang, Li-Na;Fang, Wei;Chen, Xiang-Long;Wang, Yue;Cao, Bao-Shuai;Chen, Gang-Ying;Zhu, Yi-Jing;Gu, Jun;Chen, Jian-Guo;,期刊：Journal of Medicinal Chemistry, 页码：718-725 , 文章类型： 研究论文，,卷期：2009年52-3]
- A series of novel poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors were designed within 2-aminothiazole analogs based on a constructed three-dimensional pharmacophore model. Then, the inhibitory effect on PARP-1 activi...
- Design, Synthesis, and Evaluation in Vitro of Quinoline-8-carboxamides, a New Class of Poly(adenosine-diphosphate-ribose)polymerase-1 (PARP-1) Inhibitor.
[作者：Lord, Anna-Marie;Mahon, Mary F.;Lloyd, Matthew D.;Threadgill, Michael D.;,期刊：Journal of Medicinal Chemistry, 页码：868-877 , 文章类型： 研究论文，,卷期：2009年52-3]
- Poly(ADP-ribose)polymerase-1 is an important target enzyme in drug design; inhibitors have a wide variety of therapeutic activities. A series of quinoline-8-carboxamides was designed to maintain the required pharmacopho...
- Design, Synthesis, and Biological Evaluation of Fluorinated Analogues of Salicylihalamide.
[作者：Sugimoto, Yoshinori;Konoki, Keiichi;Murata, Michio;Matsushita, Masafumi;Kanazawa, Hiroshi;Oishi, Tohru;,期刊：Journal of Medicinal Chemistry, 页码：798-806 , 文章类型： 研究论文，,卷期：2009年52-3]
- Salicylihalamide A I (X = F) (SA), a benzolactone enamide compd., possesses potent cytotoxicity against human tumor cell lines. SA is a selective inhibitor of mammalian vacuolar type H+-ATPase (V-ATPase), and is distinc...
- Single-Step High-Yield Radiosynthesis and Evaluation of a Sensitive 18F-Labeled Ligand for Imaging Brain Peripheral Benzodiazepine Receptors with PET.
[作者：Briard, Emmanuelle;Zoghbi, Sami S.;Simeon, Fabrice G.;Imaizumi, Masao;Gourley, Jonathan P.;Shetty, H. Umesha;Lu, Shuiyu;Fujita, Masahiro;Innis, Robert B.;Pike, Victor W.;,期刊：Journal of Medicinal Chemistry, 页码：688-699 , 文章类型： 研究论文，,卷期：2009年52-3]
- Elevated levels of peripheral benzodiazepine receptors (PBR) are assocd. with activated microglia in their response to inflammation. Hence, PBR imaging in vivo is valuable for investigating brain inflammatory conditions....
- Modeling binding modes of a7 nicotinic acetylcholine receptor with ligands: the roles of Gln117 and other residues of the receptor in agonist binding.
[作者：Huang, Xiaoqin;Zheng, Fang;Stokes, Clare;Papke, Roger L.;Zhan, Chang-Guo;,期刊：Journal of Medicinal Chemistry, 页码：890-890 , 文章类型： 研究论文，,卷期：2009年52-3]
- On page 6300, in the right column, in the Acknowledgment section, the NIH grants supporting the work are Grants U19DA017548 and R01GM57481. The correct version of the Acknowledgment section, is given.
- Prodrugs of Perzinfotel with Improved Oral Bioavailability.
[作者：Baudy, Reinhardt B.;Butera, John A.;Abou-Gharbia, Magid A.;Chen, Hong;Harrison, Boyd;Jain, Uday;Magolda, Ronald;Sze, Jean Y.;Brandt, Michael R.;Cummons, Terri A.;Kowal, Diane;Pangalos, Menelas N.;Zupan, Bojana;Hoffmann, Matthew;May, Michael;Mugford, Chery,期刊：Journal of Medicinal Chemistry, 页码：771-778 , 文章类型： 研究论文，,卷期：2009年52-3]
- Previous studies with perzinfotel, a potent, selective, competitive NMDA receptor antagonist, showed it to be efficacious in inflammatory and neuropathic pain models. To increase the low oral bioavailability of perzinfo...
- Design, Synthesis, and Evaluation of Oxygen-Containing Macrocyclic Peptidomimetics as Inhibitors of HCV NS3 Protease.
[作者：Velazquez, Francisco;Venkatraman, Srikanth;Blackman, Melissa;Pinto, Patrick;Bogen, Stephane;Sannigrahi, Mousumi;Chen, Kevin;Pichardo, John;Hart, Andrea;Tong, Xiao;Girijavallabhan, Viyyoor;Njoroge, F. George;,期刊：Journal of Medicinal Chemistry, 页码：700-708 , 文章类型： 研究论文，,卷期：2009年52-3]
- HCV infection is considered a silent epidemic because most people infected do not develop acute symptoms. Instead, the disease progresses to a chronic state leading to cirrhosis and hepatocarcinoma. Novel therapies are...
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