- Design, Synthesis, and Biological Evaluation of a Series of 2-Hydroxyisoquinoline-1,3(2H,4H)-diones as Dual Inhibitors of Human Immunodeficiency Virus Type 1 Integrase and the Reverse Transcriptase RNase H Domain.
[作者:Billamboz, Muriel;Bailly, Fabrice;Barreca, Maria Letizia;De Luca, Laura;Mouscadet, Jean-Francois;Calmels, Christina;Andreola, Marie-Line;Witvrouw, Myriam;Christ, Frauke;Debyser, Zeger;Cotelle, Philippe;,期刊:Journal of Medicinal Chemistry, 页码:7717-7730 , 文章类型: 研究论文,,卷期:2008年51-24]
- The synthesis of a series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones I (R = H, NO2, Cl, Br, I, OH, NHCOMe, 4-HCC6h4, etc.) variously substituted at the position 7 aimed at inhibiting selectively two-metal ion catalytic a...
- Synthesis and Anticancer Activity Comparison of Phenylalkyl Isoselenocyanates with Corresponding Naturally Occurring and Synthetic Isothiocyanates.
[作者:Sharma, Arun K.;Sharma, Arati;Desai, Dhimant;Madhunapantula, SubbaRao V.;Huh, Sung Jin;Robertson, Gavin P.;Amin, Shantu;,期刊:Journal of Medicinal Chemistry, 页码:7820-7826 , 文章类型: 研究论文,,卷期:2008年51-24]
- Synthesis and identification of novel phenylalkyl isoselenocyanates (ISCs), isosteric selenium analogs of naturally occurring phenylalkyl isothiocyanates (ITCs), as effective cytotoxic and antitumor agents are described....
- Development and Preclinical Studies of Broad-Spectrum Anti-HIV Agent (3'R,4'R)-3-Cyanomethyl-4-methyl-3',4'-di-O-(S)-camphanoyl-(+)-cis-kh ellactone (3-Cyanomethyl-4-methyl-DCK).
[作者:Xie, Lan;Guo, Huan-Fang;Lu, Hong;Zhuang, Xiao-Mei;Zhang, An-Ming;Wu, Gang;Ruan, Jin-Xiu;Zhou, Ting;Yu, Donglei;Qian, Keduo;Lee, Kuo-Hsiung;Jiang, Shibo;,期刊:Journal of Medicinal Chemistry, 页码:7689-7696 , 文章类型: 研究论文,,卷期:2008年51-24]
- In prior investigation, we discovered that (3'R,4'R)-3-cyanomethyl-4-methyl-3',4'-di-O-(S)-camphanoyl-(+)-cis-khe llactone [I (R = (S)-camphanoyl), 3-cyanomethyl-4-methyl-DCK] showed promising anti-HIV activity. In thes...
- New Analgesics Synthetically Derived from the Paracetamol Metabolite N-(4-Hydroxyphenyl)-(5Z,8Z,11Z,14Z)-icosatetra-5,8,11,14-enamide.
[作者:Sinning, Christian;Watzer, Bernhard;Coste, Ovidiu;Nuesing, Rolf M.;Ott, Ingo;Ligresti, Alessia;Di Marzo, Vincenzo;Imming, Peter;,期刊:Journal of Medicinal Chemistry, 页码:7800-7805 , 文章类型: 研究论文,,卷期:2008年51-24]
- N-(4-Hydroxyphenyl)-(5Z,8Z,11Z,14Z)-icosatetra-5,8,11,14-enamide (AM404) is a metabolite of the well-known analgesic paracetamol. AM404 inhibits endocannabinoid cellular uptake, binds weakly to CB1 and CB2 cannabinoid re...
- Synthesis and Structure-Activity Relationships of 2-Amino-1-aroylnaphthalene and 2-Hydroxy-1-aroylnaphthalenes as Potent Antitubulin Agents.
[作者:Reddy, Gadarla Randheer;Kuo, Ching-Chuan;Tan, Uan-Kang;Coumar, Mohane Selvaraj;Chang, Chi-Yen;Chiang, Yi-Kun;Lai, Mei-Jung;Yeh, Jiann-Yih;Wu, Su-Ying;Chang, Jang-Yang;Liou, Jing-Ping;Hsieh, Hsing-Pang;,期刊:Journal of Medicinal Chemistry, 页码:8163-8167 , 文章类型: 研究论文,,卷期:2008年51-24]
- A series of aroylnaphthalenes were prepd. as bioisosteres of combrestatin A-4 and evaluated for anticancer activity. Aroylnaphthalenes I (R = HO, H2N) showed strong antiproliferative activity with IC50 values of 2.1-26.3...
- Synthesis of Polyfluoro Ketones for Selective Inhibition of Human Phospholipase A2 Enzymes.
[作者:Baskakis, Constantinos;Magrioti, Victoria;Cotton, Naomi;Stephens, Daren;Constantinou-Kokotou, Violetta;Dennis, Edward A.;Kokotos, George;,期刊:Journal of Medicinal Chemistry, 页码:8027-8037 , 文章类型: 研究论文,,卷期:2008年51-24]
- The development of selective inhibitors for individual PLA2 enzymes is necessary in order to target PLA2-specific signaling pathways, but it is challenging due to the obsd. promiscuity of known PLA2 inhibitors. This wor...
- Structural and Mechanistic Studies of Mofegiline Inhibition of Recombinant Human Monoamine Oxidase B.
[作者:Milczek, Erika M.;Bonivento, Daniele;Binda, Claudia;Mattevi, Andrea;McDonald, Ian A.;Edmondson, Dale E.;,期刊:Journal of Medicinal Chemistry, 页码:8019-8026 , 文章类型: 研究论文,,卷期:2008年51-24]
- Mechanistic and structural studies have been carried out to investigate the mol. basis for the irreversible inhibition of human MAO-B by mofegiline. Competitive inhibition with substrate shows an apparent Ki of 28 nM. ...
- Type-II Kinase Inhibitor Docking, Screening, and Profiling Using Modified Structures of Active Kinase States.
[作者:Kufareva, Irina;Abagyan, Ruben;,期刊:Journal of Medicinal Chemistry, 页码:7921-7932 , 文章类型: 研究论文,,卷期:2008年51-24]
- Type-II kinase inhibitors represent a class of chems. that trap their target kinases in an inactive, so-called DFG-out state, occupying a hydrophobic pocket adjacent to the ATP binding site. These compds. are often more...
- Identification of Potent, Selective, and Metabolically Stable Peptide Antagonists to the Calcitonin Gene-Related Peptide (CGRP) Receptor.
[作者:Miranda, Les P.;Holder, Jerry Ryan;Shi, Licheng;Bennett, Brian;Aral, Jennifer;Gegg, Colin V.;Wright, Marie;Walker, Kenneth;Doellgast, George;Rogers, Rick;Li, Hongyan;Valladares, Violeta;Salyers, Kevin;Johnson, Eileen;Wild, Kenneth;,期刊:Journal of Medicinal Chemistry, 页码:7889-7897 , 文章类型: 研究论文,,卷期:2008年51-24]
- Calcitonin gene-related peptide (CGRP) is a 37-residue neuropeptide that can be converted to a CGRP1 receptor antagonist by the truncation of its first seven residues. CGRP(8-37), 1, has a CGRP1 receptor Ki = 3.2 nM but ...
- Orally Bioavailable Isothioureas Block Function of the Chemokine Receptor CXCR4 In Vitro and In Vivo.
[作者:Thoma, Gebhard;Streiff, Markus B.;Kovarik, Jiri;Glickman, Fraser;Wagner, Trixie;Beerli, Christian;Zerwes, Hans-Gunter;,期刊:Journal of Medicinal Chemistry, 页码:7915-7920 , 文章类型: 研究论文,,卷期:2008年51-24]
- The interaction of the chemokine receptor CXCR4 with its ligand CXCL12 is involved in many biol. processes such as hematopoiesis, migration of immune cells, as well as in cancer metastasis. CXCR4 also mediates the infec...
- Aryl Bis(diazeniumdiolates): Potent Inducers of S-Glutathionylation of Cellular Proteins and Their in Vitro Antiproliferative Activities.
[作者:Andrei, Daniela;Maciag, Anna E.;Chakrapani, Harinath;Citro, Michael L.;Keefer, Larry K.;Saavedra, Joseph E.;,期刊:Journal of Medicinal Chemistry, 页码:7944-7952 , 文章类型: 研究论文,,卷期:2008年51-24]
- A no. of bis(diazeniumdiolates) that we designed to release up to 4 mol of nitric oxide (NO) and that are structural analogs of the NO prodrug and anticancer lead compd. O2-{2,4-dinitro-5-[4-(N-methylamino)benzoyloxy]phe...
- The Fourth Molybdenum Containing Enzyme mARC: Cloning and Involvement in the Activation of N-Hydroxylated Prodrugs.
[作者:Gruenewald, Sanja;Wahl, Bettina;Bittner, Florian;Hungeling, Helen;Kanzow, Stephanie;Kotthaus, Joscha;Schwering, Ulrike;Mendel, Ralf R.;Clement, Bernd;,期刊:Journal of Medicinal Chemistry, 页码:8173-8177 , 文章类型: 研究论文,,卷期:2008年51-24]
- The recently discovered mammalian molybdoprotein mARC1 is capable of reducing N-hydroxylated compds. Upon reconstitution with cytochrome b5 and b5 reductase, benzamidoxime, pentamidine, and diminazene amidoximes, N-hydr...
- Citrullination of Linear and Cyclic Altered Peptide Ligands from Myelin Basic Protein (MBP87-99) Epitope Elicits a Th1 Polarized Response by T Cells Isolated from Multiple Sclerosis Patients: Implications in Triggering Disease.
[作者:Deraos, George;Chatzantoni, Kokona;Matsoukas, Minos-Timotheos;Tselios, Theodore;Deraos, Spyros;Katsara, Maria;Papathanasopoulos, Panagiotis;Vynios, Demitrios;Apostolopoulos, Vasso;Mouzaki, Athanasia;Matsoukas, John;,期刊:Journal of Medicinal Chemistry, 页码:7834-7842 , 文章类型: 研究论文,,卷期:2008年51-24]
- Derangement of cellular immunity is central in the pathophysiol. of multiple sclerosis (MS) and is often manifested by abnormal cytokine prodn. The authors investigated cytokine secretion in peripheral blood mononuclear...
- Improving Tumor Uptake and Excretion Kinetics of 99mTc-Labeled Cyclic Arginine-Glycine-Aspartic (RGD) Dimers with Triglycine Linkers.
[作者:Shi, Jiyun;Wang, Lijun;Kim, Young-Seung;Zhai, Shizhen;Liu, Zhaofei;Chen, Xiaoyuan;Liu, Shuang;,期刊:Journal of Medicinal Chemistry, 页码:7980-7990 , 文章类型: 研究论文,,卷期:2008年51-24]
- This report describes the synthesis of two new cyclic RGD (Arg-Gly-Asp) dimers, 3 (E[G3-c(RGDfK)]2) and 4 (G3-E[G3-c(RGDfK)]2), and their corresponding conjugates 5 (HYNIC-E[G3-c(RGDfK)]2: HYNIC = 6-(2-(2-sulfonatobenzal...
- Engineering Stabilized Vascular Endothelial Growth Factor-A Antagonists: Synthesis, Structural Characterization, and Bioactivity of Grafted Analogues of Cyclotides.
[作者:Gunasekera, Sunithi;Foley, Fiona M.;Clark, Richard J.;Sando, Lillian;Fabri, Louis J.;Craik, David J.;Daly, Norelle L.;,期刊:Journal of Medicinal Chemistry, 页码:7697-7704 , 文章类型: 研究论文,,卷期:2008年51-24]
- Cyclotides are plant derived mini-proteins with compact folded structures and exceptional stability. Their stability derives from a head-to-tail cyclized backbone coupled with a cystine knot arrangement of three-conserv...
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