- Chemically Induced Dimerization of Human Nonpancreatic Secretory Phospholipase A2 by Bis-indole Derivatives.
[作者:Zhou, Lu;Fang, Chao;Wei, Ping;Liu, Shiyong;Liu, Ying;Lai, Luhua;,期刊:Journal of Medicinal Chemistry, 页码:3360-3366 , 文章类型: 研究论文,,卷期:2008年51-12]
- A series of novel bis-indole compds., 1,w-bis(((3-acetamino-5-methoxy-2-methylindole)-2-methylene)phenoxy )alkane I [X = (CH2)n, n= 3-9], have been designed and synthesized on the basis of the enzyme structure of human n...
- Synthesis and Evaluation of Estrogen Agonism of Diaryl 4,5-Dihydroisoxazoles, 3-Hydroxyketones, 3-Methoxyketones, and 1,3-Diketones: A Compound Set Forming a 4D Molecular Library.
[作者:Pulkkinen, Juha T.;Honkakoski, Paavo;Perakyla, Mikael;Berczi, Istvan;Laatikainen, Reino;,期刊:Journal of Medicinal Chemistry, 页码:3562-3571 , 文章类型: 研究论文,,卷期:2008年51-12]
- Derivatives, and Condensed Benzenoid Compounds) Section In this paper, the prepn. and systematic evaluation of estrogen receptor a (ERa) and estrogen receptor b (ERb) activities of some diaryl-1,3-diones, e.g. PhCOCH2COC...
- Triazolopyrimidine-Based Dihydroorotate Dehydrogenase Inhibitors with Potent and Selective Activity against the Malaria Parasite Plasmodium falciparum.
[作者:Phillips, Margaret A.;Gujjar, Ramesh;Malmquist, Nicholas A.;White, John;El Mazouni, Farah;Baldwin, Jeffrey;Rathod, Pradipsinh K.;,期刊:Journal of Medicinal Chemistry, 页码:3649-3653 , 文章类型: 研究论文,,卷期:2008年51-12]
- A Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitor I that is potent (KI = 15 nM) and species-selective (>5000-fold over the human enzyme) was identified by high-throughput screening. The substituted...
- New C5-Alkylated Indolobenzazepinones Acting as Inhibitors of Tubulin Polymerization: Cytotoxic and Antitumor Activities.
[作者:Keller, Laurent;Beaumont, Stephane;Liu, Jian-Miao;Thoret, Sylviane;Bignon, Jerome S.;Wdzieczak-Bakala, Joanna;Dauban, Philippe;Dodd, Robert H.;,期刊:Journal of Medicinal Chemistry, 页码:3414-3421 , 文章类型: 研究论文,,卷期:2008年51-12]
- A series of 5-alkylindolobenzazepin-7-ones was synthesized by Suzuki coupling between 3-iodoindole-2-carboxylates and the appropriate a-alkylbenzylamino o-boronic acids followed by cyclization to the lactam. Derivs. hav...
- 1,5-Diphenylpyrrole Derivatives as Antimycobacterial Agents. Probing the Influence on Antimycobacterial Activity of Lipophilic Substituents at the Phenyl Rings.
[作者:Biava, Mariangela;Porretta, Giulio Cesare;Poce, Giovanna;De Logu, Alessandro;Saddi, Manuela;Meleddu, Rita;Manetti, Fabrizio;De Rossi, Edda;Botta, Maurizio;,期刊:Journal of Medicinal Chemistry, 页码:3644-3648 , 文章类型: 研究论文,,卷期:2008年51-12]
- Synthesis and biol. evaluation of new derivs. (e.g. I) of 1,5-bis(4-chlorophenyl)-2-methyl-3-(4-methylpiperazin-1-yl)methyl-1H-p yrrole (BM 212) are reported. Variously substituted Ph rings with different substitution p...
- Clavatadine A, A Natural Product with Selective Recognition and Irreversible Inhibition of Factor XIa.
[作者:Buchanan, Malcolm S.;Carroll, Anthony R.;Wessling, Deborah;Jobling, Michael;Avery, Vicky M.;Davis, Rohan A.;Feng, Yunjiang;Xue, Yafeng;Oster, Linda;Fex, Tomas;Deinum, Johanna;Hooper, John N. A.;Quinn, Ronald J.;,期刊:Journal of Medicinal Chemistry, 页码:3583-3587 , 文章类型: 研究论文,,卷期:2008年51-12]
- Bioassay-guided fractionation of a CH2Cl2/MeOH ext. of the sponge Suberea clavata using the serine protease factor XIa to detect antithrombotic activity led to the isolation of the new marine natural products, clavatadin...
- Homology Modeling and Site-Directed Mutagenesis To Identify Selective Inhibitors of Endothelin-Converting Enzyme-2.
[作者:Gagnidze, Khatuna;Sachchidanand;Rozenfeld, Raphael;Mezei, Mihaly;Zhou, Ming-Ming;Devi, Lakshmi A.;,期刊:Journal of Medicinal Chemistry, 页码:3378-3387 , 文章类型: 研究论文,,卷期:2008年51-12]
- Endothelin-converting enzyme-2 (ECE-2), a member of M13 family of zinc metallopeptidases, has previously been shown to process a no. of neuropeptides including those derived from prodynorphin, proenkephalin, proSAAS, and...
- Conjugation of Poly-L-lysine to Bacterial Cytosine Deaminase Improves the Efficacy of Enzyme/Prodrug Cancer Therapy.
[作者:Li, Cong;Wildes, Flonne;Winnard, Paul, Jr.;Artemov, Dmitri;Penet, Marie-France;Bhujwalla, Zaver M.;,期刊:Journal of Medicinal Chemistry, 页码:3572-3582 , 文章类型: 研究论文,,卷期:2008年51-12]
- We previously obsd. that bacterial cytosine deaminase (bCD) demonstrated high therapeutic efficacy in an enzyme/prodrug cancer therapeutic strategy. To understand the role of polycationic PLL in the cellular uptake of b...
- Novel Donepezil-Based Inhibitors of Acetyl- and Butyrylcholinesterase and Acetylcholinesterase-Induced b-Amyloid Aggregation.
[作者:Camps, Pelayo;Formosa, Xavier;Galdeano, Carles;Gomez, Tania;Munoz-Torrero, Diego;Scarpellini, Michele;Viayna, Elisabet;Badia, Albert;Clos, M. Victoria;Camins, Antoni;Pallas, Merce;Bartolini, Manuela;Mancini, Francesca;Andrisano, Vincenza;Estelrich, Joan;L,期刊:Journal of Medicinal Chemistry, 页码:3588-3598 , 文章类型: 研究论文,,卷期:2008年51-12]
- simultaneously interact with the active, peripheral and midgorge binding sites of acetylcholinesterase (AChE) have been synthesized and tested for their ability to inhibit AChE, butyrylcholinesterase (BChE), and AChE-ind...
- Naturally Occurring Pentacyclic Triterpenes as Inhibitors of Glycogen Phosphorylase: Synthesis, Structure-Activity Relationships, and X-ray Crystallographic Studies.
[作者:Wen, Xiaoan;Sun, Hongbin;Liu, Jun;Cheng, Keguang;Zhang, Pu;Zhang, Liying;Hao, Jia;Zhang, Luyong;Ni, Peizhou;Zographos, Spyros E.;Leonidas, Demetres D.;Alexacou, Kyra-Melinda;Gimisis, Thanasis;Hayes, Joseph M.;Oikonomakos, Nikos G.;,期刊:Journal of Medicinal Chemistry, 页码:3540-3554 , 文章类型: 研究论文,,卷期:2008年51-12]
- Twenty-five naturally occurring pentacyclic triterpenes, 15 of which were synthesized in this study, were biol. evaluated as inhibitors of rabbit muscle glycogen phosphorylase a (GPa). From SAR studies, the presence of ...
- 1-[(Imidazolidin-2-yl)imino]indazole. Highly a2/I1 Selective Agonist: Synthesis, X-ray Structure, and Biological Activity.
[作者:Saczewski, Franciszek;Kornicka, Anita;Rybczynska, Apolonia;Hudson, Alan L.;Miao, Shu Sean;Gdaniec, Maria;Boblewski, Konrad;Lehmann, Artur;,期刊:Journal of Medicinal Chemistry, 页码:3599-3608 , 文章类型: 研究论文,,卷期:2008年51-12]
- (Heterocyclic Compounds (More Than One Hetero Atom)) Section Novel benzazole derivs. bearing a (imidazolidin-2-yl)imino moiety at position 1 or 2 were synthesized by reacting 1-amino- or 2-aminobenzazoles with N,N'-bis(t...
- Discovery of Imidazo[1,5-c]imidazol-3-ones: Weakly Basic, Orally Active Factor Xa Inhibitors.
[作者:Imaeda, Yasuhiro;Kuroita, Takanobu;Sakamoto, Hiroki;Kawamoto, Tetsuji;Tobisu, Mamoru;Konishi, Noriko;Hiroe, Katsuhiko;Kawamura, Masaki;Tanaka, Toshimasa;Kubo, Keiji;,期刊:Journal of Medicinal Chemistry, 页码:3422-3436 , 文章类型: 研究论文,,卷期:2008年51-12]
- The coagulation enzyme factor Xa (FXa) has been recognized as a promising target for the development of new antithrombotic agents. We previously found I to be an orally bioavailable FXa inhibitor in fasted monkeys; howev...
- Designing selective, high affinity ligands of 5-HT1D receptor by covalent dimerization of 5-HT1F ligands derived from 4-fluoro-N-[3-(1-methyl-4-piperidinyl)-1H-indol-5-yl]benzamide.
[作者:Choi, Seok-Ki;Green, David;Ho, Anne;Klein, Uwe;Marquess, Daniel;Taylor, Robert;Turner, S. Derek;,期刊:Journal of Medicinal Chemistry, 页码:3609-3616 , 文章类型: 研究论文,,卷期:2008年51-12]
- We demonstrate here that covalent dimerization of 5-HT1 ligands is an effective design strategy to modulate affinity and selectivity of 5-HT1 ligands. This approach was applied to LY-334370, a selective agonist of 5-HT1...
- Conformationally Constrained Analogues of N-(Piperidinyl)-5-(4-Chlorophenyl)-1-(2,4- Dichlorophenyl)-4-Methyl-1H-Pyrazole-3-Carboxamide (SR141716): Design, Synthesis, Computational Analysis, And Biological Evaluations.
[作者:Zhang, Yanan;Burgess, Jason P.;Brackeen, Marcus;Gilliam, Anne;Mascarella, S. Wayne;Page, Kevin;Seltzman, Herbert H.;Thomas, Brian F.;,期刊:Journal of Medicinal Chemistry, 页码:3526-3539 , 文章类型: 研究论文,,卷期:2008年51-12]
- Structure-activity relationships of the title compd. I have been extensively documented, but the conformational properties of this class have received less attention. In an attempt to better understand ligand conformati...
- Synthesis and Biological Evaluation of D-Amino Acid Oxidase Inhibitors.
[作者:Ferraris, Dana;Duvall, Bridget;Ko, Yao-Sen;Thomas, Ajit G.;Rojas, Camilo;Majer, Pavel;Hashimoto, Kenji;Tsukamoto, Takashi;,期刊:Journal of Medicinal Chemistry, 页码:3357-3359 , 文章类型: 研究论文,,卷期:2008年51-12]
- D-Amino acid oxidase (DAAO) catalyzes the oxidn. of D-amino acids including D-serine, a full agonist at the glycine site of the NMDA receptor. A series of benzo[d]isoxazol-3-ol derivs. were synthesized and evaluated as ...
- Synthesis, Cytotoxicity, DNA Interaction, and Topoisomerase II Inhibition Properties of Novel Indeno[2,1-c]quinolin-7-one and Indeno[1,2-c]isoquinolin-5,11-dione Derivatives.
[作者:Ryckebusch, Adina;Garcin, Deborah;Lansiaux, Amelie;Goossens, Jean-Francois;Baldeyrou, Brigitte;Houssin, Raymond;Bailly, Christian;Henichart, Jean-Pierre;,期刊:Journal of Medicinal Chemistry, 页码:3617-3629 , 文章类型: 研究论文,,卷期:2008年51-12]
- (Heterocyclic Compounds (One Hetero Atom)) Section Indeno[2,1-c]quinolin-7-ones and 6H-indeno[1,2-c]isoquinoline-5,11-diones, bearing two cationic aminoalkyl side chains, were synthesized and evaluated for DNA interactio...
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