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Publikationer i urvalet

28 träffar

Bibliografisk träff 2024-07-23

Discovery of ZJCK-6-46: A Potent, Selective, and Orally Available Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A Inhibitor for the Treatment of Alzheimer's Disease.

Chen H, Gao X, Li X, Yu C, Liu W, Qiu J, Liu W, Geng H, Zheng F, Gong H, Xu Z, Jia J, Zhao Q.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.4c00483

Bibliografisk träff 2023-11-10

HDAC specificity and kinase off-targeting by purine-benzohydroxamate anti-hematological tumor agents.

Waitman KB, de Almeida LC, Primi MC, Carlos JAEG, Ruiz C, Kronenberger T, Laufer S, Goettert MI, Poso A, Vassiliades SV, de Souza VAM, Toledo MFZJ, Hassimotto NMA, Cameron MD, Bannister TD, Costa-Lotufo LV, Machado-Neto JA, Tavares MT, Parise-Filho R.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2023.115935

Bibliografisk träff 2023-06-19

Discovery of orally active sulfonylphenyl thieno[3,2-d]pyrimidine derivatives as GPR119 agonists.

Kim H, Kim M, Oh K, Lee S, Lim S, Lee S, Kim YH, Suh KH, Min KH.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2023.115584

Bibliografisk träff 2019-11-19

Development of Robust 17(<i>R</i>),18(<i>S</i>)-Epoxyeicosatetraenoic Acid (17,18-EEQ) Analogues as Potential Clinical Antiarrhythmic Agents.

Adebesin AM, Wesser T, Vijaykumar J, Konkel A, Paudyal MP, Lossie J, Zhu C, Westphal C, Puli N, Fischer R, Schunck WH, Falck JR.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.9b00952

Bibliografisk träff 2019-01-28

Evaluation of Amides, Carbamates, Sulfonamides, and Ureas of 4-Prop-2-ynylidenecycloalkylamine as Potent, Selective, and Bioavailable Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5.

Graziani D, Caligari S, Callegari E, De Toma C, Longhi M, Frigerio F, Dilernia R, Menegon S, Pinzi L, Pirona L, Tazzari V, Valsecchi AE, Vistoli G, Rastelli G, Riva C.

J Med Chem · journal article · DOI 10.1021/acs.jmedchem.8b01226

Bibliografisk träff 2019-01-23

Design, Synthesis, and Biological Evaluation of New 1-(Aryl-1 H-pyrrolyl)(phenyl)methyl-1 H-imidazole Derivatives as Antiprotozoal Agents.

Saccoliti F, Madia VN, Tudino V, De Leo A, Pescatori L, Messore A, De Vita D, Scipione L, Brun R, Kaiser M, Mäser P, Calvet CM, Jennings GK, Podust LM, Pepe G, Cirilli R, Faggi C, Di Marco A, Battista MR, Summa V, Costi R, Di Santo R.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.8b01464

Bibliografisk träff 2018-08-02

Design, synthesis and biological evaluation of a series of novel GPR40 agonists containing nitrogen heterocyclic rings.

Sun Z, Zhou T, Pan X, Yang Y, Huan Y, Xiao Z, Shen Z, Liu Z.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2018.07.048

Bibliografisk träff 2018-05-17

Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.

O' Neill PM, Stocks PA, Sabbani S, Roberts NL, Amewu RK, Shore ER, Aljayyoussi G, Angulo-Barturén I, Belén M, Jiménez-Díaz, Bazaga SF, Martínez MS, Campo B, Sharma R, Charman SA, Ryan E, Chen G, Shackleford DM, Davies J, Nixon GL, Biagini GA, Ward SA.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2018.05.006

Bibliografisk träff 2017-01-23

Discovery of GBT440, an Orally Bioavailable R-State Stabilizer of Sickle Cell Hemoglobin.

Metcalf B, Chuang C, Dufu K, Patel MP, Silva-Garcia A, Johnson C, Lu Q, Partridge JR, Patskovska L, Patskovsky Y, Almo SC, Jacobson MP, Hua L, Xu Q, Gwaltney SL, Yee C, Harris J, Morgan BP, James J, Xu D, Hutchaleelaha A, Paulvannan K, Oksenberg D, Li Z.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.6b00491

Bibliografisk träff 2016-03-28

2-hydroxyisoquinoline-1,3(2H,4H)-diones (HIDs) as human immunodeficiency virus type 1 integrase inhibitors: Influence of the alkylcarboxamide substitution of position 4.

Billamboz M, Suchaud V, Bailly F, Lion C, Andréola ML, Christ F, Debyser Z, Cotelle P.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2016.03.083

Bibliografisk träff 2016-03-23

Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism.

Carosati E, Cosimelli B, Ioan P, Severi E, Katneni K, Chiu FC, Saponara S, Fusi F, Frosini M, Matucci R, Micucci M, Chiarini A, Spinelli D, Budriesi R.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.6b00030

Bibliografisk träff 2015-08-10

A Ligand-Based Drug Design. Discovery of 4-Trifluoromethyl-7,8-pyranocoumarin as a Selective Inhibitor of Human Cytochrome P450 1A2.

Liu J, Pham PT, Skripnikova EV, Zheng S, Lovings LJ, Wang Y, Goyal N, Bellow SM, Mensah LM, Chatters AJ, Bratton MR, Wiese TE, Zhao M, Wang G, Foroozesh M.

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/acs.jmedchem.5b00494

Bibliografisk träff 2015-08-04

Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM).

Elkamhawy A, Viswanath AN, Pae AN, Kim HY, Heo JC, Park WK, Lee CO, Yang H, Kim KH, Nam DH, Seol HJ, Cho H, Roh EJ.

Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2015.08.001

Bibliografisk träff 2015-07-10

4-Fluoro-3',4',5'-trimethoxychalcone as a new anti-invasive agent. From discovery to initial validation in an in vivo metastasis model.

Roman BI, De Ryck T, Patronov A, Slavov SH, Vanhoecke BW, Katritzky AR, Bracke ME, Stevens CV.

Eur J Med Chem · research support, non-u.s. gov't; validation study; journal article · DOI 10.1016/j.ejmech.2015.06.029

Bibliografisk träff 2014-07-18

Discovery of novel pyrimidine and malonamide derivatives as TGR5 agonists.

Park EJ, Ahn YG, Jung SH, Bang HJ, Kim M, Hong DJ, Kim J, Suh KH, Kim YJ, Kim D, Kim EY, Lee K, Min KH.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2014.07.026

Bibliografisk träff 2014-05-14

Investigation of a novel series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones as human immunodeficiency virus type 1 integrase inhibitors.

Suchaud V, Bailly F, Lion C, Calmels C, Andréola ML, Christ F, Debyser Z, Cotelle P.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm500109z

Bibliografisk träff 2013-09-30

Rational development of 4-aminopyridyl-based inhibitors targeting Trypanosoma cruzi CYP51 as anti-chagas agents.

Choi JY, Calvet CM, Gunatilleke SS, Ruiz C, Cameron MD, McKerrow JH, Podust LM, Roush WR.

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/jm401067s

Bibliografisk träff 2012-05-15

Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.

Karlgren M, Vildhede A, Norinder U, Wisniewski JR, Kimoto E, Lai Y, Haglund U, Artursson P.

J Med Chem · research support, non-u.s. gov't; research-article; journal article · DOI 10.1021/jm300212s

Bibliografisk träff 2011-03-08

Fine-tuning the selectivity of aldosterone synthase inhibitors: structure-activity and structure-selectivity insights from studies of heteroaryl substituted 1,2,5,6-tetrahydropyrrolo[3,2,1-ij]quinolin-4-one derivatives.

Lucas S, Negri M, Heim R, Zimmer C, Hartmann RW.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm101470k

Bibliografisk träff 2010-12-28

New drug-like hydroxyphenylnaphthol steroidomimetics as potent and selective 17β-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of estrogen-dependent diseases.

Marchais-Oberwinkler S, Wetzel M, Ziegler E, Kruchten P, Werth R, Henn C, Hartmann RW, Frotscher M.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm1009082

Bibliografisk träff 2010-11-24

CYP1A2-mediated biotransformation of cardioactive 2-thienylidene-3,4-methylenedioxybenzoylhydrazine (LASSBio-294) by rat liver microsomes and human recombinant CYP enzymes.

Fraga AG, da Silva LL, Fraga CA, Barreiro EJ.

Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2010.11.024

Bibliografisk träff 2008-12-01

In vivo active aldosterone synthase inhibitors with improved selectivity: lead optimization providing a series of pyridine substituted 3,4-dihydro-1H-quinolin-2-one derivatives.

Lucas S, Heim R, Ries C, Schewe KE, Birk B, Hartmann RW.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm800888q

Bibliografisk träff 2008-09-03

Novel aldosterone synthase inhibitors with extended carbocyclic skeleton by a combined ligand-based and structure-based drug design approach.

Lucas S, Heim R, Negri M, Antes I, Ries C, Schewe KE, Bisi A, Gobbi S, Hartmann RW.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm800683c

Bibliografisk träff 2008-08-01

Overcoming undesirable CYP1A2 inhibition of pyridylnaphthalene-type aldosterone synthase inhibitors: influence of heteroaryl derivatization on potency and selectivity.

Heim R, Lucas S, Grombein CM, Ries C, Schewe KE, Negri M, Müller-Vieira U, Birk B, Hartmann RW.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm800377h

Bibliografisk träff 2008-03-07

Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent diseases.

Frotscher M, Ziegler E, Marchais-Oberwinkler S, Kruchten P, Neugebauer A, Fetzer L, Scherer C, Müller-Vieira U, Messinger J, Thole H, Hartmann RW.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm701447v

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 2006-11-01

OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.

Matsumoto M, Hashizume H, Tomishige T, Kawasaki M, Tsubouchi H, Sasaki H, Shimokawa Y, Komatsu M.

PLoS Med · research support, non-u.s. gov't; research-article; journal article · DOI 10.1371/journal.pmed.0030466

Bibliografisk träff 2005-10-01

Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.

Fontana E, Dansette PM, Poli SM.

Curr Drug Metab · systematic review; journal article · DOI 10.2174/138920005774330639