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Publikationer i urvalet

50 träffar

Bibliografisk träff 2013-10-08

3,5-bis(benzylidene)-4-piperidones and related N-acyl analogs: a novel cluster of antimalarials targeting the liver stage of Plasmodium falciparum.

Das U, Singh RS, Alcorn J, Hickman MR, Sciotti RJ, Leed SE, Lee PJ, Roncal N, Dimmock JR.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2013.09.065

Bibliografisk träff 2013-10-01

Synthesis and in vitro and in vivo pharmacological evaluation of new 4-aminoquinoline-based compounds.

Tukulula M, Njoroge M, Abay ET, Mugumbate GC, Wiesner L, Taylor D, Gibhard L, Norman J, Swart KJ, Gut J, Rosenthal PJ, Barteau S, Streckfuss J, Kameni-Tcheudji J, Chibale K.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/ml400311r

Bibliografisk träff 2013-07-12

4-Amino-7-chloroquinolines: probing ligand efficiency provides botulinum neurotoxin serotype A light chain inhibitors with significant antiprotozoal activity.

Opsenica IM, Tot M, Gomba L, Nuss JE, Sciotti RJ, Bavari S, Burnett JC, Solaja BA.

J Med Chem · research support, non-u.s. gov't; research-article; research support, u.s. gov't, non-p.h.s.; journal article; research support, n.i.h., extramural · DOI 10.1021/jm4006077

Bibliografisk träff 2013-04-09

Structure-based identification of OATP1B1/3 inhibitors.

De Bruyn T, van Westen GJ, Ijzerman AP, Stieger B, de Witte P, Augustijns PF, Annaert PP.

Mol Pharmacol · research support, non-u.s. gov't; journal article · DOI 10.1124/mol.112.084152

Bibliografisk träff 2011-12-09

Design and synthesis of small molecular dual inhibitor of falcipain-2 and dihydrofolate reductase as antimalarial agent.

Huang H, Lu W, Li X, Cong X, Ma H, Liu X, Zhang Y, Che P, Ma R, Li H, Shen X, Jiang H, Huang J, Zhu J.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2011.12.011

Bibliografisk träff 2010-09-15

A predictive ligand-based Bayesian model for human drug-induced liver injury.

Ekins S, Williams AJ, Xu JJ.

Drug Metab Dispos · journal article · DOI 10.1124/dmd.110.035113

Bibliografisk träff 2010-07-21

Structure-activity relationships of mononuclear metal-thiosemicarbazone complexes endowed with potent antiplasmodial and antiamoebic activities.

Bahl D, Athar F, Soares MB, de Sá MS, Moreira DR, Srivastava RM, Leite AC, Azam A.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2010.07.039

Bibliografisk träff 2010-07-01

Developing structure-activity relationships for the prediction of hepatotoxicity.

Greene N, Fisk L, Naven RT, Note RR, Patel ML, Pelletier DJ.

Chem Res Toxicol · journal article · DOI 10.1021/tx1000865

Bibliografisk träff 2010-06-14

Discovery of potent small-molecule inhibitors of multidrug-resistant Plasmodium falciparum using a novel miniaturized high-throughput luciferase-based assay.

Lucumi E, Darling C, Jo H, Napper AD, Chandramohanadas R, Fisher N, Shone AE, Jing H, Ward SA, Biagini GA, DeGrado WF, Diamond SL, Greenbaum DC.

Antimicrob Agents Chemother · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1128/aac.00431-10

Bibliografisk träff 2010-05-26

Synthesis of novel alpha-pyranochalcones and pyrazoline derivatives as Plasmodium falciparum growth inhibitors.

Wanare G, Aher R, Kawathekar N, Ranjan R, Kaushik NK, Sahal D.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2010.05.069

Bibliografisk träff 2010-05-15

In vitro and in vivo antimalarial evaluation of semi-synthetic derivatives of gomphostenin.

Sathe M, Kaushik MP.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2010.05.035

Bibliografisk träff 2010-05-01

Thousands of chemical starting points for antimalarial lead identification.

Gamo FJ, Sanz LM, Vidal J, de Cozar C, Alvarez E, Lavandera JL, Vanderwall DE, Green DV, Kumar V, Hasan S, Brown JR, Peishoff CE, Cardon LR, Garcia-Bustos JF.

Nature · research support, non-u.s. gov't; journal article · DOI 10.1038/nature09107

Bibliografisk träff 2010-01-01

Modular synthesis and in vitro and in vivo antimalarial assessment of C-10 pyrrole mannich base derivatives of artemisinin.

Pacorel B, Leung SC, Stachulski AV, Davies J, Vivas L, Lander H, Ward SA, Kaiser M, Brun R, O'Neill PM.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm901216v

Bibliografisk träff 2009-12-11

Synthesis and evaluation of phenylequine for antimalarial activity in vitro and in vivo.

Blackie MA, Yardley V, Chibale K.

Bioorg Med Chem Lett · comparative study; research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2009.12.030

Bibliografisk träff 2009-11-11

A 4-aminoquinoline derivative that markedly sensitizes tumor cell killing by Akt inhibitors with a minimum cytotoxicity to non-cancer cells.

Hu C, Raja Solomon V, Cano P, Lee H.

Eur J Med Chem · research support, non-u.s. gov't; research-article; journal article · DOI 10.1016/j.ejmech.2009.11.017

Bibliografisk träff 2009-10-28

Synthesis and antimalarial evaluation of 1, 3, 5-trisubstituted pyrazolines.

Acharya BN, Saraswat D, Tiwari M, Shrivastava AK, Ghorpade R, Bapna S, Kaushik MP.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2009.10.023

Bibliografisk träff 2009-09-06

Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.

Yuan J, Johnson RL, Huang R, Wichterman J, Jiang H, Hayton K, Fidock DA, Wellems TE, Inglese J, Austin CP, Su XZ.

Nat Chem Biol · research support, n.i.h., intramural; research-article; journal article; research support, n.i.h., extramural · DOI 10.1038/nchembio.215

Bibliografisk träff 2009-06-08

Antiviral activity of chloroquine against human coronavirus OC43 infection in newborn mice.

Keyaerts E, Li S, Vijgen L, Rysman E, Verbeeck J, Van Ranst M, Maes P.

Antimicrob Agents Chemother · research support, non-u.s. gov't; research-article; journal article · DOI 10.1128/aac.01509-08

Bibliografisk träff 2009-04-01

Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.

O'Neill PM, Shone AE, Stanford D, Nixon G, Asadollahy E, Park BK, Maggs JL, Roberts P, Stocks PA, Biagini G, Bray PG, Davies J, Berry N, Hall C, Rimmer K, Winstanley PA, Hindley S, Bambal RB, Davis CB, Bates M, Gresham SL, Brigandi RA, Gomez-de-Las-Heras FM, Gargallo DV, Parapini S, Vivas L, Lander H, Taramelli D, Ward SA.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm8012757

Bibliografisk träff 2008-10-31

New antimalarial and cytotoxic 4-nerolidylcatechol derivatives.

Pinto AC, Silva LF, Cavalcanti BC, Melo MR, Chaves FC, Lotufo LV, de Moraes MO, de Andrade-Neto VF, Tadei WP, Pessoa CO, Vieira PP, Pohlit AM.

Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2008.10.025

Bibliografisk träff 2008-09-17

New ferrocenic pyrrolo[1,2-a]quinoxaline derivatives: synthesis, and in vitro antimalarial activity.

Guillon J, Moreau S, Mouray E, Sinou V, Forfar I, Fabre SB, Desplat V, Millet P, Parzy D, Jarry C, Grellier P.

Bioorg Med Chem · journal article · DOI 10.1016/j.bmc.2008.09.038

Bibliografisk träff 2008-07-29

The efficacy and selectivity of tumor cell killing by Akt inhibitors are substantially increased by chloroquine.

Hu C, Solomon VR, Ulibarri G, Lee H.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2008.07.076

Bibliografisk träff 2008-05-16

Antimalarial activity of novel pyrrolizidinyl derivatives of 4-aminoquinoline.

Sparatore A, Basilico N, Casagrande M, Parapini S, Taramelli D, Brun R, Wittlin S, Sparatore F.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2008.05.042

Bibliografisk träff 2008-04-14

First case of emergence of atovaquone-proguanil resistance in Plasmodium falciparum during treatment in a traveler in Comoros.

Savini H, Bogreau H, Bertaux L, Bouchiba H, Kraemer P, Parzy D, Garnotel E, Rogier C, Simon F, Pradines B.

Antimicrob Agents Chemother · letter; research support, non-u.s. gov't; case reports · DOI 10.1128/aac.00282-08

Bibliografisk träff 2008-04-09

Synthesis and structure-activity relationships of 4-pyridones as potential antimalarials.

Yeates CL, Batchelor JF, Capon EC, Cheesman NJ, Fry M, Hudson AT, Pudney M, Trimming H, Woolven J, Bueno JM, Chicharro J, Fernández E, Fiandor JM, Gargallo-Viola D, Gómez de las Heras F, Herreros E, León ML.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm0705760

Bibliografisk träff 2008-02-14

Combining HPLC-PDA-MS-SPE-NMR with circular dichroism for complete natural product characterization in crude extracts: levorotatory gossypol in Thespesia danis.

Sprogøe K, Staek D, Ziegler HL, Jensen TH, Holm-Møller SB, Jaroszewski JW.

J Nat Prod · journal article · DOI 10.1021/np800010r

Bibliografisk träff 2007-10-14

Pharmacomodulation on the 3-acetylursolic acid skeleton: Design, synthesis, and biological evaluation of novel N-{3-[4-(3-aminopropyl)piperazinyl]propyl}-3-O-acetylursolamide derivatives as antimalarial agents.

Gnoatto SC, Susplugas S, Dalla Vechia L, Ferreira TB, Dassonville-Klimpt A, Zimmer KR, Demailly C, Da Nascimento S, Guillon J, Grellier P, Verli H, Gosmann G, Sonnet P.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2007.10.031

Bibliografisk träff 2007-04-08

Chemical genetics reveals a complex functional ground state of neural stem cells.

Diamandis P, Wildenhain J, Clarke ID, Sacher AG, Graham J, Bellows DS, Ling EK, Ward RJ, Jamieson LG, Tyers M, Dirks PB.

Nat Chem Biol · research support, non-u.s. gov't; journal article · DOI 10.1038/nchembio873

Bibliografisk träff 2007-01-12

Comparison of a SYBR green I-based assay with a histidine-rich protein II enzyme-linked immunosorbent assay for in vitro antimalarial drug efficacy testing and application to clinical isolates.

Bacon DJ, Latour C, Lucas C, Colina O, Ringwald P, Picot S.

Antimicrob Agents Chemother · comparative study; research-article; research support, u.s. gov't, non-p.h.s.; journal article · DOI 10.1128/aac.01313-06

Bibliografisk träff 2005-04-01

Synthesis of some cryptolepine analogues, assessment of their antimalarial and cytotoxic activities, and consideration of their antimalarial mode of action.

Onyeibor O, Croft SL, Dodson HI, Feiz-Haddad M, Kendrick H, Millington NJ, Parapini S, Phillips RM, Seville S, Shnyder SD, Taramelli D, Wright CW.

J Med Chem · journal article · DOI 10.1021/jm040893w