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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44条记录   Potent Dual Thymidylate Synthase and Dihydrofolate Reductase Inhibitors: Classical and Nonclassical 2-Amino-4-oxo-5-arylthio-substituted-6-methylthieno[2,3-d]pyrimidine Antifolates. [作者：Gangjee, Aleem;Qiu, Yibin;Li, Wei;Kisliuk, Roy L.;,期刊：Journal of Medicinal Chemistry, 页码：5789-5797 , 文章类型： 研究论文，,卷期：2008年51-18] N-{4-[(2-Amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)s ulfanyl]benzoyl}-L-glutamic acid (I) and nine nonclassical analogs II (R = Ph, 4-Cl-Ph, 4-NO2-Ph, 2,5-di-OMe-Ph, 3,4-di-Cl-Ph, 3,5-di-Cl-Ph, 2-naphth... Synthesis and Biological Evaluation of 2-Amino-3-(4-Chlorobenzoyl)-4-[N-(Substituted) Piperazin-1-yl]Thiophenes as Potent Allosteric Enhancers of the A1 Adenosine Receptor. [作者：Romagnoli, Romeo;Baraldi, Pier Giovanni;Carrion, Maria Dora;Cara, Carlota Lopez;Cruz-Lopez, Olga;Iaconinoto, Maria Antonietta;Preti, Delia;Shryock, John C.;Moorman, Allan R.;Vincenzi, Fabrizio;Varani, Katia;Andrea Borea, Pier;,期刊：Journal of Medicinal Chemistry, 页码：5875-5879 , 文章类型： 研究论文，,卷期：2008年51-18] The synthesis and evaluation of a series of 2-amino-3-(4-chlorobenzoyl)-4-[4-(alkyl/aryl)piperazin-yl]thiophene derivs. as allosteric enhancers of the A1-adenosine receptor are described. The nature of substituents on t... The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morph olin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer. [作者：Folkes, Adrian J.;Ahmadi, Khatereh;Alderton, Wendy K.;Alix, Sonia;Baker, Stewart J.;Box, Gary;Chuckowree, Irina S.;Clarke, Paul A.;Depledge, Paul;Eccles, Suzanne A.;Friedman, Lori S.;Hayes, Angela;Hancox, Timothy C.;Kugendradas, Arumugam;Lensun, Letitia;M,期刊：Journal of Medicinal Chemistry, 页码：5522-5532 , 文章类型： 研究论文，,卷期：2008年51-18] Compounds (More Than One Hetero Atom)) Section Phosphatidylinositol-3-kinase (PI3K) is an important target in cancer due to the deregulation of the PI3K/Akt signaling pathway in a wide variety of tumors. A series of thi... Discovery of Antimycobacterial Spiro-piperidin-4-ones: An Atom Economic, Stereoselective Synthesis, and Biological Intervention. [作者：Kumar, Raju Ranjith;Perumal, Subbu;Senthilkumar, Palaniappan;Yogeeswari, Perumal;Sriram, Dharmarajan;,期刊：Journal of Medicinal Chemistry, 页码：5731-5735 , 文章类型： 研究论文，,卷期：2008年51-18] An atom economic and stereoselective synthesis of several spiro-piperidin-4-ones through 1,3-dipolar cycloaddn. of azomethine ylides generated in situ from isatin and a-amino acids viz. proline, phenylglycine, and sarcos... Anxiolytic-like Effects of N,N-Dialkyl-2-phenylindol-3-ylglyoxylamides by Modulation of Translocator Protein Promoting Neurosteroid Biosynthesis. [作者：Da Settimo, Federico;Simorini, Francesca;Taliani, Sabrina;La Motta, Concettina;Marini, Anna Maria;Salerno, Silvia;Bellandi, Marusca;Novellino, Ettore;Greco, Giovanni;Cosimelli, Barbara;Da Pozzo, Eleonora;Costa, Barbara;Simola, Nicola;Morelli, Micaela;Mart,期刊：Journal of Medicinal Chemistry, 页码：5798-5806 , 文章类型： 研究论文，,卷期：2008年51-18] Novel N,N-disubstituted indol-3-ylglyoxylamides, bearing different combinations of substituents R1-R5, were synthesized and evaluated as ligands of the translocator protein (TSPO), the 18 kDa protein representing the min... 3,4-Dihydro-2H-1,4-benzoxazine Derivatives Combining Thrombin Inhibitory and Glycoprotein IIb/IIIa Receptor Antagonistic Activity as a Novel Class of Antithrombotic Compounds with Dual Function. [作者：Ilas, Janez;Jakopin, Ziga;Borstnar, Tina;Stegnar, Mojca;Kikelj, Danijel;,期刊：Journal of Medicinal Chemistry, 页码：5617-5629 , 文章类型： 研究论文，,卷期：2008年51-18] (Heterocyclic Compounds (More Than One Hetero Atom)) Section 3,4-Dihydro-2H-1,4-benzoxazines, e.g. I [6- or 7-substitution; R1 = H, PhCH2, PhCO, 2-pyridylmethyl; R2 = H, R3O2CCH2, EtO2CCO, R3O2CCH2CH2, PhCH2CH(CO2R3)CO; ... Genome-Wide Computational and Expression Analyses Reveal G-Quadruplex DNA Motifs as Conserved cis-Regulatory Elements in Human and Related Species. [作者：Verma, Anjali;Halder, Kangkan;Halder, Rashi;Yadav, Vinod Kumar;Rawal, Pooja;Thakur, Ram Krishna;Mohd, Farhan;Sharma, Abhay;Chowdhury, Shantanu;,期刊：Journal of Medicinal Chemistry, 页码：5641-5649 , 文章类型： 研究论文，,卷期：2008年51-18] Using a combination of in silico and exptl. approaches, we present evidence that the G-quadruplex (G4) motif (an alternative higher-order DNA conformation) has regulatory potential. Genome-wide analyses of 99980 human, ... Identification of 4-(2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl] oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a Novel Inhibitor of AKT Kinase. [作者：Heerding, Dirk A.;Rhodes, Nelson;Leber, Jack D.;Clark, Tammy J.;Keenan, Richard M.;Lafrance, Louis V.;Li, Mei;Safonov, Igor G.;Takata, Dennis T.;Venslavsky, Joseph W.;Yamashita, Dennis S.;Choudhry, Anthony E.;Copeland, Robert A.;Lai, Zhihong;Schaber, Mich,期刊：Journal of Medicinal Chemistry, 页码：5663-5679 , 文章类型： 研究论文，,卷期：2008年51-18] and expression of dominant neg. AKT blocks the ability of a variety of growth factors to promote survival. Therefore, inhibitors of AKT kinase activity might be useful as monotherapy for the treatment of tumors with act... Structural Modifications of N-(1,2,3,4-Tetrahydronaphthalen-1-yl)-4-Aryl-1-piperazinehexanamides : Influence on Lipophilicity and 5-HT7 Receptor Activity. Part III. [作者：Leopoldo, Marcello;Lacivita, Enza;De Giorgio, Paola;Fracasso, Claudia;Guzzetti, Sara;Caccia, Silvio;Contino, Marialessandra;Colabufo, Nicola A.;Berardi, Francesco;Perrone, Roberto;,期刊：Journal of Medicinal Chemistry, 页码：5813-5822 , 文章类型： 研究论文，,卷期：2008年51-18] Starting from the previously reported 5-HT7 receptor agents 4-7 with N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamide structure, the 1-(2-methylthiophenyl)-, 1-(2-diphenyl)-, 1-(2-isopropylphenyl)-, an... Mixed-Lineage Kinase 1 and Mixed-Lineage Kinase 3 Subtype-Selective Dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: Optimization, Mixed-Lineage Kinase 1 Crystallography, and Oral in Vivo Activity in 1-Methyl-4-phenyltetrahydropyridine Models. [作者：Hudkins, Robert L.;Diebold, James L.;Tao, Ming;Josef, Kurt A.;Park, Chung Ho;Angeles, Thelma S.;Aimone, Lisa D.;Husten, Jean;Ator, Mark A.;Meyer, Sheryl L.;Holskin, Beverly P.;Durkin, John T.;Fedorov, Alexander A.;Fedorov, Elena V.;Almo, Steven C.;Mathias,期刊：Journal of Medicinal Chemistry, 页码：5680-5689 , 文章类型： 研究论文，,卷期：2008年51-18] The optimization of the dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-one R2 and R12 positions led to the identification of the first MLK1 and MLK3 subtype-selective inhibitors within the MLK family. Compds. 14 (CEP-5... Discovery of Novel Cdc25 Phosphatase Inhibitors with Micromolar Activity Based on the Structure-Based Virtual Screening. [作者：Park, Hwangseo;Bahn, Young Jae;Jung, Suk-Kyeong;Jeong, Dae Gwin;Lee, Sang-Hyeup;Seo, Il;Yoon, Tae-Sung;Kim, Seung Jun;Ryu, Seong Eon;,期刊：Journal of Medicinal Chemistry, 页码：5533-5541 , 文章类型： 研究论文，,卷期：2008年51-18] Cdc25 phosphatases have been considered as attractive drug targets for anticancer therapy because of the correlation of their overexpression with a wide variety of cancers. We have been able to identify five novel Cdc25... 4''-Benzoylureido-TSAO Derivatives as Potent and Selective Non-Nucleoside HCMV Inhibitors. Structure-Activity Relationship and Mechanism of Antiviral Action. [作者：de Castro, Sonia;Peromingo, M. Teresa;Naesens, Lieve;Andrei, Graciela;Snoeck, Robert;Balzarini, Jan;Velazquez, Sonsoles;Camarasa, Maria-Jose;,期刊：Journal of Medicinal Chemistry, 页码：5823-5832 , 文章类型： 研究论文，,卷期：2008年51-18] Analogs of the 4''-benzoyl-ureido-TSAO deriv. (1) modified at different positions have been prepd. and evaluated against wild-type strains of HCMV and murine cytomegalovirus (MCMV) in cell culture. In addn., the activit... Novel Insight in Structure-Activity Relationship and Bioanalysis of P-Glycoprotein Targeting Highly Potent Tetrakishydroxymethyl Substituted 3,9-Diazatetraasteranes. [作者：Coburger, Claudius;Wollmann, Jorg;Baumert, Christiane;Krug, Martin;Molnar, Josef;Lage, Hermann;Hilgeroth, Andreas;,期刊：Journal of Medicinal Chemistry, 页码：5871-5874 , 文章类型： 研究论文，,卷期：2008年51-18] (Heterocyclic Compounds (More Than One Hetero Atom)) Section Novel 3,9-diazatetraasteranes, e.g. I, were synthesized with varied inhibitors. Structure-activity relationships (SAR) were discussed in relation to detd. phy... Discovery of Orally Bioavailable Cathepsin S Inhibitors for the Reversal of Neuropathic Pain. [作者：Irie, Osamu;Kosaka, Takatoshi;Ehara, Takeru;Yokokawa, Fumiaki;Kanazawa, Takanori;Hirao, Hajime;Iwasaki, Astuko;Sakaki, Junichi;Teno, Naoki;Hitomi, Yuko;Iwasaki, Genji;Fukaya, Hiroaki;Nonomura, Kazuhiko;Tanabe, Keiko;Koizumi, Shinichi;Uchiyama, Noriko;Beva,期刊：Journal of Medicinal Chemistry, 页码：5502-5505 , 文章类型： 研究论文，,卷期：2008年51-18] Cathepsin S inhibitors are well-known to be an attractive target as immunol. therapeutic agents. Recently, our gene expression anal. identified that cathepsin S inhibitors could also be effective for neuropathic pain. ... Enantiomeric Propanolamines as selective N-Methyl-D-aspartate 2B Receptor Antagonists. [作者：Tahirovic, Yesim A.;Geballe, Matthew;Gruszecka-Kowalik, Ewa;Myers, Scott J.;Lyuboslavsky, Polina;Le, Phuong;French, Adam;Irier, Hasan;Choi, Woo-baeg;Easterling, Keith;Yuan, Hongjie;Wilson, Lawrence J.;Kotloski, Robert;McNamara, James O.;Dingledine, Raymon,期刊：Journal of Medicinal Chemistry, 页码：5506-5521 , 文章类型： 研究论文，,卷期：2008年51-18] Enantiomeric propanolamines have been identified as a new class of NR2B-selective NMDA receptor antagonists. The most effective agents are biaryl structures, synthesized in six steps with overall yields ranging from 11-... Virtual Screening, Identification, and Biochemical Characterization of Novel Inhibitors of the Reverse Transcriptase of Human Immunodeficiency Virus Type-1. [作者：Herschhorn, Alon;Hizi, Amnon;,期刊：Journal of Medicinal Chemistry, 页码：5702-5713 , 文章类型： 研究论文，,卷期：2008年51-18] The reverse transcriptase (RT) of human immunodeficiency virus type-1 (HIV-1) is a leading target in current antiretroviral therapy. Unfortunately, drug-resistant RT mutants evolve under the pressure of these drugs, and ...