- Salicylanilides: Selective inhibitors of interleukin-12p40 production.
[作者:Brown, Michael E.;Fitzner, Jeffrey N.;Stevens, Tracey;Chin, Wilson;Wright, Clifford D.;Boyce, Jim P.;,期刊:Bioorganic & Medicinal Chemistry, 页码:8760-8764 , 文章类型: 研究论文,,卷期:2008年16-18]
- Interleukin (IL)-12p40, a subunit component of both IL-12 and IL-23, is being widely studied for its role in inflammatory disease. As part of an effort to profile cellular signaling pathways across different cell types,...
- Development and biological evaluation of C60 fulleropyrrolidine-thalidomide dyad as a new anti-inflammation agent.
[作者:Huang, Sheng-Tung;Ho, Chia-Shin;Lin, Chun-Mao;Fang, Hsu-Wei;Peng, Yi-Xiang;,期刊:Bioorganic & Medicinal Chemistry, 页码:8619-8626 , 文章类型: 研究论文,,卷期:2008年16-18]
- increased due to the broad range of biol. activities that were found for these compds. The authors designed and prepd. a new C60 fullerene hybrid bearing thalidomide as a potential double-action anti-inflammatory agent,...
- Design and synthesis of 6-fluoro-2-naphthyl derivatives as novel CCR3 antagonists with reduced CYP2D6 inhibition.
[作者:Sato, Ippei;Morihira, Koichiro;Inami, Hiroshi;Kubota, Hirokazu;Morokata, Tatsuaki;Suzuki, Keiko;Iura, Yosuke;Nitta, Aiko;Imaoka, Takayuki;Takahashi, Toshiya;Takeuchi, Makoto;Ohta, Mitsuaki;Tsukamoto, Shin-ichi;,期刊:Bioorganic & Medicinal Chemistry, 页码:8607-8618 , 文章类型: 研究论文,,卷期:2008年16-18]
- In our previous study on discovering novel types of CCR3 antagonists, we found a fluoronaphthalene deriv. (1) that exhibited potent CCR3 inhibitory activity with an IC50 value of 20 nM. However, compd. 1 also inhibited ...
- Conjugates of the fungal cytotoxin illudin M with improved tumor specificity.
[作者:Schobert, Rainer;Biersack, Bernhard;Knauer, Sebastian;Ocker, Matthias;,期刊:Bioorganic & Medicinal Chemistry, 页码:8592-8597 , 文章类型: 研究论文,,卷期:2008年16-18]
- A simplified procedure for the isolation of gram quantities of illudin M from culture broths of basidiomycete Omphalotus olearius is described. Esters of illudin M with docosahexaenoic acid, chlorambucil, demethylcanthar...
- 11-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine derivatives as novel topoisomerase I-targeting agents.
[作者:Feng, Wei;Satyanarayana, Mavurapu;Tsai, Yuan-Chin;Liu, Angela A.;Liu, Leroy F.;LaVoie, Edmond J.;,期刊:Bioorganic & Medicinal Chemistry, 页码:8598-8606 , 文章类型: 研究论文,,卷期:2008年16-18]
- Several 11-substituted benzo[i]phenanthridine derivs. were synthesized, and their TOP1-targeting activity and cytotoxicity were assessed. Comparative data indicate that TOP1-targeting was often the primary mol. target a...
- Nucleosides and oligonucleotides containing 1,2,3-triazole residues with nucleobase tethers: Synthesis via the azide-alkyne 'click' reaction.
[作者:Chittepu, Padmaja;Sirivolu, Venkata Ramana;Seela, Frank;,期刊:Bioorganic & Medicinal Chemistry, 页码:8427-8439 , 文章类型: 研究论文,,卷期:2008年16-18]
- were prepd. via copper(I)-catalyzed 1,3-dipolar cycloaddn. of N-9 propargylpurines or N-1 propargylpyrimidines with the toluoyl protected 1-azido-2-deoxyribofuranose followed by treatment with NaOMe/MeOH or aq NH3. The ...
- Novel iron complexes bearing N6-substituted adenosine derivatives: Synthesis, magnetic, 57Fe Moessbauer, DFT, and in vitro cytotoxicity studies.
[作者:Travnicek, Zdenek;Mikulik, Jiri;Cajan, Michal;Zboril, Radek;Popa, Igor;,期刊:Bioorganic & Medicinal Chemistry, 页码:8719-8728 , 文章类型: 研究论文,,卷期:2008年16-18]
- predominant compn. [Fe(L n)Cl3] ?H2O {where L1 = N6-(2-fluorobenzyl)adenosine (1), L2 = N6-(4-fluorobenzyl)adenosine (2), L3 = N6-(2-trifluoromethylbenzyl)adenosine (3), L4 = N6-(3-trifluoromethylbenzyl)adenosine (4), L5...
- Synthesis, biological evaluation and SAR study of novel pyrazole analogues as inhibitors of Mycobacterium tuberculosis.
[作者:Castagnolo, Daniele;De Logu, Alessandro;Radi, Marco;Bechi, Beatrice;Manetti, Fabrizio;Magnani, Matteo;Supino, Sibilla;Meleddu, Rita;Chisu, Lorenza;Botta, Maurizio;,期刊:Bioorganic & Medicinal Chemistry, 页码:8587-8591 , 文章类型: 研究论文,,卷期:2008年16-18]
- As a continuation of the previous work that turned toward the identification of antimycobacterial compds. with innovative structures, two series of pyrazole derivs. were synthesized by parallel soln.-phase synthesis and ...
- Achiral oligoamines as versatile tool for the development of aspartic protease inhibitors.
[作者:Blum, Andreas;Boettcher, Jark;Sammet, Benedikt;Luksch, Torsten;Heine, Andreas;Klebe, Gerhard;Diederich, Wibke E.;,期刊:Bioorganic & Medicinal Chemistry, 页码:8574-8586 , 文章类型: 研究论文,,卷期:2008年16-18]
- Due to the important role that aspartic proteases play in many patho-physiol. processes, they have intensively been targeted by modern drug development. However, up to now, only for two family members, renin and HIV pro...
- N-Propylnoraporphin-11-O-yl carboxylic esters as potent dopamine D2 and serotonin 5-HT1A receptor dual ligands.
[作者:Liu, Zhili;Chen, Xuetao;Sun, Peihua;Yu, Leiping;Zhen, Xuechu;Zhang, Ao;,期刊:Bioorganic & Medicinal Chemistry, 页码:8335-8338 , 文章类型: 研究论文,,卷期:2008年16-18]
- A small series of N-propylnoraporphin-11-O-yl carboxylic esters with variant ester lengths were synthesized and their binding potencies at were evaluated. Monoesters 3a-f showed binding potency of 100 nM or less for the...
- Tetrahydropyridine-4-carboxamides as novel, potent transient receptor potential vanilloid 1 (TRPV1) antagonists.
[作者:Brown, Brian S.;Keddy, Ryan;Zheng, Guo Zhu;Schmidt, Robert G.;Koenig, John R.;McDonald, Heath A.;Bianchi, Bruce R.;Honore, Prisca;Jarvis, Michael F.;Surowy, Carol S.;Polakowski, James S.;Marsh, Kennan C.;Faltynek, Connie R.;Lee, Chih-Hung;,期刊:Bioorganic & Medicinal Chemistry, 页码:8516-8525 , 文章类型: 研究论文,,卷期:2008年16-18]
- 6(I), have been synthesized and evaluated for in vitro TRPV1 antagonist activity, and in vivo analgesic activity in animal pain models. The tetrahydropyridine 6 is a novel TRPV1 receptor antagonist that potently inhibit...
- Synthesis of new indeno[1,2-e]pyrimido[4,5-b][1,4]diazepine-5,11-diones as potential antitumor agents.
[作者:Insuasty, Braulio;Orozco, Fabian;Lizarazo, Carolina;Quiroga, Jairo;Abonia, Rodrigo;Hursthouse, Mike;Nogueras, Manuel;Cobo, Justo;,期刊:Bioorganic & Medicinal Chemistry, 页码:8492-8500 , 文章类型: 研究论文,,卷期:2008年16-18]
- 3-29 were obtained regioselectivity from the reaction of 5,6-diamino-3,4-dihydropyrimidin-4-ones 1 and 2-arylideneindandiones 2 as reagents. These compds. have been evaluated at the US National Cancer Institute (NCI) fo...
- Design, synthesis, and biological evaluation of new mitonafide derivatives as potential antitumor drugs.
[作者:Antonini, Ippolito;Volpini, Rosaria;Dal Ben, Diego;Lambertucci, Catia;Cristalli, Gloria;,期刊:Bioorganic & Medicinal Chemistry, 页码:8440-8446 , 文章类型: 研究论文,,卷期:2008年16-18]
- A series of potential DNA-binding antitumor agents, 2-[w-(alkylamino)alkyl]-6-{[w-(alkylamino)alkyl]amino}-1H-benzo[de]isoq uinolin-1,3(2H)-diones and 1,7-bis{6-[(w-(dimethylamino)alkyl)amino]-1,3-dioxo-1H-benzo[de]isoqu...
- Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-N,N-dimethylamino benzo[b]furan derivatives as inhibitors of tubulin polymerization.
[作者:Romagnoli, Romeo;Baraldi, Pier Giovanni;Sarkar, Taradas;Carrion, Maria Dora;Cruz-Lopez, Olga;Lopez Cara, Carlota;Tolomeo, Manlio;Grimaudo, Stefania;Di Cristina, Antonietta;Pipitone, Maria Rosaria;Balzarini, Jan;Gambari, Roberto;Ilaria, Lampronti;Saletti,,期刊:Bioorganic & Medicinal Chemistry, 页码:8419-8426 , 文章类型: 研究论文,,卷期:2008年16-18]
- cancer. A new class of inhibitors of tubulin polymn. based on the 2-(3,4,5-trimethoxybenzoyl)-2-dimethylamino-benzo[b]furan mol. skeleton was synthesized and evaluated for antiproliferative activity, inhibition of tubul...
- Oleanolic acid and its derivatives: New inhibitor of protein tyrosine phosphatase 1B with cellular activities.
[作者:Zhang, Yi-Nan;Zhang, Wei;Hong, Di;Shi, Lei;Shen, Qiang;Li, Jing-Ya;Li, Jia;Hu, Li-Hong;,期刊:Bioorganic & Medicinal Chemistry, 页码:8697-8705 , 文章类型: 研究论文,,卷期:2008年16-18]
- Protein tyrosine phosphatase 1B is a key factor in the neg. regulation of insulin pathway and a promising target for treatment of diabetes and obesity. Herein, a series of competitive inhibitors were optimized from olea...
- Synthesis, biological active molecular design, and molecular docking study of novel deazaflavin-cholestane hybrid compounds.
[作者:Shrestha, Ajaya R.;Shindo, Takashi;Ashida, Noriyuki;Nagamatsu, Tomohisa;,期刊:Bioorganic & Medicinal Chemistry, 页码:8685-8696 , 文章类型: 研究论文,,卷期:2008年16-18]
- Novel deazaflavin-cholestane hybrid compds., 3',8'-disubstituted-5'-deazacholest-2,4-dieno[2,3-g]pteridine-2',4'(3'H,8' H)-diones, have been synthesized by condensation reaction between 6-(monosubstituted amino)-pyrimidi...
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