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Publikationer i urvalet

41 träffar

Bibliografisk träff 2024-01-13

Identification and evaluation of small-molecule inhibitors against the dNTPase SAMHD1 via a comprehensive screening funnel.

Zhang SM, Paulin CBJ, Shu H, Yagüe-Capilla M, Michel M, Marttila P, Ortis F, Bwanika HC, Dirks C, Venkatram RP, Wiita E, Jemth AS, Almlöf I, Loseva O, Hormann FM, Koolmeister T, Linde E, Lee S, Llona-Minguez S, Haraldsson M, Axelsson H, Strömberg K, Homan EJ, Scobie M, Lundbäck T, Helleday T, Rudd SG.

iScience · research-article; journal article · DOI 10.1016/j.isci.2024.108907

Bibliografisk träff 2023-07-19

A preclinical secondary pharmacology resource illuminates target-adverse drug reaction associations of marketed drugs.

Sutherland JJ, Yonchev D, Fekete A, Urban L.

Nat Commun · research support, non-u.s. gov't; research-article; journal article · DOI 10.1038/s41467-023-40064-9

Bibliografisk träff 2016-03-12

Synthesis, characterization and biological evaluation of benzothiazoles and tetrahydrobenzothiazoles bearing urea or thiourea moieties as vasorelaxants and inhibitors of the insulin releasing process.

Harrouche K, Renard JF, Bouider N, de Tullio P, Goffin E, Lebrun P, Faury G, Pirotte B, Khelili S.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2016.03.028

Bibliografisk träff 2014-01-31

Microwave-assisted synthesis and myorelaxant activity of 9-indolyl-1,8-acridinedione derivatives.

Gündüz MG, Işli F, El-Khouly A, Yıldırım S, Öztürk Fincan GS, Şimşek R, Şafak C, Sarıoğlu Y, Öztürk Yıldırım S, Butcher RJ.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2014.01.059

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 2012-09-07

Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.

Warner DJ, Chen H, Cantin LD, Kenna JG, Stahl S, Walker CL, Noeske T.

Drug Metab Dispos · journal article · DOI 10.1124/dmd.112.047068

Bibliografisk träff 2012-07-04

N-Aryl-N'-(chroman-4-yl)ureas and thioureas display in vitro anticancer activity and selectivity on apoptosis-resistant glioblastoma cells: screening, synthesis of simplified derivatives, and structure-activity relationship analysis.

Goffin E, Lamoral-Theys D, Tajeddine N, de Tullio P, Mondin L, Lefranc F, Gailly P, Rogister B, Kiss R, Pirotte B.

Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2012.06.050

Bibliografisk träff 2012-05-15

Synthesis and pharmacological activity of N-(2,2-dimethyl-3,4-dihydro-2H-1-benzopyran-4-yl)-4H-1,2,4-benzothiadiazine-3-carboxamides 1,1-dioxides on rat uterus, rat aorta and rat pancreatic β-cells.

Khelili S, Kihal N, Yekhlef M, de Tullio P, Lebrun P, Pirotte B.

Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2012.05.011

Bibliografisk träff 2011-12-15

Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).

Liu Z, Shi Q, Ding D, Kelly R, Fang H, Tong W.

PLoS Comput Biol · research support, u.s. gov't, p.h.s.; research-article; journal article · DOI 10.1371/journal.pcbi.1002310

Bibliografisk träff 2011-09-30

In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.

Dawson S, Stahl S, Paul N, Barber J, Kenna JG.

Drug Metab Dispos · comparative study; journal article · DOI 10.1124/dmd.111.040758

Bibliografisk träff 2011-04-08

Impact of the nature of the substituent at the 3-position of 4H-1,2,4-benzothiadiazine 1,1-dioxides on their opening activity toward ATP-sensitive potassium channels.

Pirotte B, de Tullio P, Boverie S, Michaux C, Lebrun P.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm200100c

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 2010-07-01

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 2010-01-01

Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.

Fourches D, Barnes JC, Day NC, Bradley P, Reed JZ, Tropsha A.

Chem Res Toxicol · research-article; research support, u.s. gov't, non-p.h.s.; journal article; research support, n.i.h., extramural · DOI 10.1021/tx900326k

Bibliografisk träff 2009-09-25

New R/S-3,4-dihydro-2,2-dimethyl-2H-1-benzopyrans as K(ATP) channel openers: modulation of the 4-position.

Florence X, Sebille S, Tullio Pd, Lebrun P, Pirotte B.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2009.09.041

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 2009-06-21

Predictive models, based on classification algorithms, for compounds potentially active as mitochondrial ATP-sensitive potassium channel openers.

Coi A, Bianucci AM, Calderone V, Testai L, Digiacomo M, Rapposelli S, Balsamo A.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2009.06.028

Bibliografisk träff 2008-11-27

Discovery and structure-activity relationships of a novel series of benzopyran-based K(ATP) openers for urge urinary incontinence.

Zhang X, Qiu Y, Li X, Bhattacharjee S, Woods M, Kraft P, Lundeen SG, Sui Z.

Bioorg Med Chem · journal article · DOI 10.1016/j.bmc.2008.11.055

Bibliografisk träff 2008-04-25

Synthesis and activity on rat aorta rings and rat pancreatic beta-cells of ring-opened analogues of benzopyran-type potassium channel activators.

Khelili S, Florence X, Bouhadja M, Abdelaziz S, Mechouch N, Mohamed Y, de Tullio P, Lebrun P, Pirotte B.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2008.04.043

Bibliografisk träff 2008-03-30

New R/S-3,4-dihydro-2,2-dimethyl-6-halo-4-(phenylaminothiocarbonylamino)-2H-1-benzopyrans structurally related to (+/-)-cromakalim as tissue-selective pancreatic beta-cell K(ATP) channel openers.

Sebille S, de Tullio P, Florence X, Becker B, Antoine MH, Michaux C, Wouters J, Pirotte B, Lebrun P.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2008.03.065

Bibliografisk träff 2007-05-13

Evaluation of myorelaxant activity of 7-substituted hexahydroquinoline derivatives in isolated rabbit gastric fundus.

Gündüz MG, Sevim Oztürk G, Vural IM, Simşek R, Sarioğlu Y, Safak C.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2007.04.012

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 2005-01-01

4,6-Disubstituted 2,2-dimethylchromans structurally related to the K(ATP) channel opener cromakalim: design, synthesis, and effect on insulin release and vascular tone.

Sebille S, de Tullio P, Becker B, Antoine MH, Boverie S, Pirotte B, Lebrun P.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm040789e

Bibliografisk träff 2004-06-01

Arylcyanoguanidines as activators of Kir6.2/SUR1K ATP channels and inhibitors of insulin release.

Tagmose TM, Schou SC, Mogensen JP, Nielsen FE, Arkhammar PO, Wahl P, Hansen BS, Worsaae A, Boonen HC, Antoine MH, Lebrun P, Hansen JB.

J Med Chem · journal article · DOI 10.1021/jm031018y

Bibliografisk träff 2003-07-01

Toward tissue-selective pancreatic B-cells KATP channel openers belonging to 3-alkylamino-7-halo-4H-1,2,4-benzothiadiazine 1,1-dioxides.

de Tullio P, Becker B, Boverie S, Dabrowski M, Wahl P, Antoine MH, Somers F, Sebille S, Ouedraogo R, Hansen JB, Lebrun P, Pirotte B.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm021117w

Bibliografisk träff 2001-08-01

Original 2-alkylamino-6-halogenoquinazolin-4(3H)-ones and K(ATP) channel activity.

Somers F, Ouedraogo R, Antoine MH, de Tullio P, Becker B, Fontaine J, Damas J, Dupont L, Rigo B, Delarge J, Lebrun P, Pirotte B.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm0004648

Bibliografisk träff 2001-07-01

Phenylcyanoguanidines as inhibitors of glucose-induced insulin secretion from beta cells.

Tagmose TM, Mogensen JP, Agerholm PC, Arkhammar PO, Wahl P, Worsaae A, Hansen JB.

Bioorg Med Chem Lett · journal article · DOI 10.1016/s0960-894x(01)00297-9

Bibliografisk träff 2000-11-01

NMR analysis of tautomerisms of active pinacidil-type potassium channel openers and a less active one.

Yoshiizumi K, Nakajima F, Kiyoi T, Kondo H.

Bioorg Med Chem Lett · journal article · DOI 10.1016/s0960-894x(00)00490-x

Bibliografisk träff 2000-04-01

3-Alkylamino-4H-pyrido[2,3-e]-1,2,4-thiadiazine 1,1-dioxides structurally related to diazoxide and pinacidil as potassium channel openers acting on vascular smooth muscle cells: design, synthesis, and pharmacological evaluation.

Pirotte B, Ouedraogo R, de Tullio P, Khelili S, Somers F, Boverie S, Dupont L, Fontaine J, Damas J, Lebrun P.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm991069o

Bibliografisk träff 2000-03-01

Design and SAR of novel potassium channel openers targeted for urge urinary incontinence. 1. N-Cyanoguanidine bioisosteres possessing in vivo bladder selectivity.

Butera JA, Antane MM, Antane SA, Argentieri TM, Freeden C, Graceffa RF, Hirth BH, Jenkins D, Lennox JR, Matelan E, Norton NW, Quagliato D, Sheldon JH, Spinelli W, Warga D, Wojdan A, Woods M.

J Med Chem · journal article · DOI 10.1021/jm9905099