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Publikationer i urvalet

21 träffar

Bibliografisk träff 2024-06-17

Discovery of novel pyrrolo[2,1-c][1,4]benzodiazepine-3,11-dione (PBD) derivatives as selective HDAC6 inhibitors for the efficient treatment of idiopathic pulmonary fibrosis (IPF) in vitro and in vivo.

Li Y, Yang H, Zhao X, Zhao X, Quan J, Wang L, Ma E, Ma C.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2024.116608

Bibliografisk träff 2024-03-15

Identification of a Novel Selective CDK9 Inhibitor for the Treatment of CRC: Design, Synthesis, and Biological Activity Evaluation.

Zhong Y, Xu J, Zhou R, Tang L, Ding S, Ren Z, Song N, Hu B, Yang H, Sun Y, Cheng M, Li J, Liu Y.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.3c02329

Bibliografisk träff 2023-06-06

Discovery of the First Potent, Selective, and In Vivo Efficacious Polo-like Kinase 4 Proteolysis Targeting Chimera Degrader for the Treatment of TRIM37-Amplified Breast Cancer.

Sun Y, Xue Y, Sun P, Mu S, Liu H, Sun Y, Wang L, Wang J, Wu T, Yin W, Qin Q, Sun Y, Liu N, Wang H, Yang H, Zhao D, Cheng M.

J Med Chem · journal article · DOI 10.1021/acs.jmedchem.3c00505

Bibliografisk träff 2023-05-31

Escaping from Flatland: Multiparameter Optimization Leads to the Discovery of Novel Tetrahydropyrido[4,3-d]pyrimidine Derivatives as Human Immunodeficiency Virus-1 Non-nucleoside Reverse Transcriptase Inhibitors with Superior Antiviral Activities against Non-nucleoside Reverse Transcriptase Inhibitor-Resistant Variants and Favorable Drug-like Profiles.

Wang Z, Sharma PP, Rathi B, Xie M, De Clercq E, Pannecouque C, Kang D, Zhan P, Liu X.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.3c00275

Bibliografisk träff 2023-02-03

Discovery of CZS-241: A Potent, Selective, and Orally Available Polo-Like Kinase 4 Inhibitor for the Treatment of Chronic Myeloid Leukemia.

Sun Y, Xue Y, Liu H, Mu S, Sun P, Sun Y, Wang L, Wang H, Wang J, Wu T, Yin W, Qin Q, Sun Y, Yang H, Zhao D, Cheng M.

J Med Chem · journal article · DOI 10.1021/acs.jmedchem.2c02124

Bibliografisk träff 2022-12-15

Identification of N- and C-3-Modified Laudanosoline Derivatives as Novel Influenza PAN Endonuclease Inhibitors.

Liao Y, Ye Y, Liu M, Liu Z, Wang J, Li B, Huo L, Zhuang Y, Chen L, Chen J, Gao Y, Ning X, Li S, Liu S, Song G.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.2c00857

Bibliografisk träff 2022-08-30

Structure-based discovery of 1-(3-fluoro-5-(5-(3-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl)phenyl)-3-(pyrimidin-5-yl)urea as a potent and selective nanomolar type-II PLK4 inhibitor.

Sun Y, Wang L, Sun Y, Wang J, Xue Y, Wu T, Yin W, Qin Q, Sun Y, Wang H, Gao Y, Yang H, Zhao D, Cheng M.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2022.114714

Bibliografisk träff 2022-08-08

Design, synthesis, and antibacterial activity of derivatives of Tryptophanyl-tRNA synthetase inhibitor indolmycin.

Sun L, Zhang S, Kou S, Yi H, Cui A, Li Z.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2022.114647

Bibliografisk träff 2020-05-12

Discovery of a non-zwitterionic oseltamivir analogue as a potent influenza a neuraminidase inhibitor.

Zhang H, Wang K, Zhu H, Zhao X, Zhao H, Lei Z, Chen B, Yang F, Liu K, Zhang K, Wang J, Tian Y.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2020.112423

Bibliografisk träff 2020-04-29

Design, Synthesis, and Mechanism Study of Benzenesulfonamide-Containing Phenylalanine Derivatives as Novel HIV-1 Capsid Inhibitors with Improved Antiviral Activities.

Sun L, Dick A, Meuser ME, Huang T, Zalloum WA, Chen CH, Cherukupalli S, Xu S, Ding X, Gao P, Kang D, De Clercq E, Pannecouque C, Cocklin S, Lee KH, Liu X, Zhan P.

J Med Chem · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.0c00015

Bibliografisk träff 2020-01-24

Design, synthesis and structure-activity relationships of 4-phenyl-1H-1,2,3-triazole phenylalanine derivatives as novel HIV-1 capsid inhibitors with promising antiviral activities.

Sun L, Huang T, Dick A, Meuser ME, Zalloum WA, Chen CH, Ding X, Gao P, Cocklin S, Lee KH, Zhan P, Liu X.

Eur J Med Chem · research-article; journal article · DOI 10.1016/j.ejmech.2020.112085

Bibliografisk träff 2019-11-19

Development of Robust 17(R),18(S)-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 2019-11-02

Design, synthesis and biological evaluation of oseltamivir derivatives containing pyridyl group as potent inhibitors of neuraminidase for influenza A.

Wang K, Lei Z, Zhao L, Chen B, Yang F, Liu K, Zhu H, Zhao H, Cao R, Zhang K, Tian Y.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2019.111841

Bibliografisk träff 2018-11-06

Structure-Based Optimization of N-Substituted Oseltamivir Derivatives as Potent Anti-Influenza A Virus Agents with Significantly Improved Potency against Oseltamivir-Resistant N1-H274Y Variant.

Zhang J, Murugan NA, Tian Y, Bertagnin C, Fang Z, Kang D, Kong X, Jia H, Sun Z, Jia R, Gao P, Poongavanam V, Loregian A, Xu W, Ma X, Ding X, Huang B, Zhan P, Liu X.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.8b01065

Bibliografisk träff 2018-07-16

Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.

Zhang J, Poongavanam V, Kang D, Bertagnin C, Lu H, Kong X, Ju H, Lu X, Gao P, Tian Y, Jia H, Desta S, Ding X, Sun L, Fang Z, Huang B, Liang X, Jia R, Ma X, Xu W, Murugan NA, Loregian A, Huang B, Zhan P, Liu X.

J Med Chem · journal article · DOI 10.1021/acs.jmedchem.8b00929

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 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 2008-01-01

Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.

Kruhlak NL, Choi SS, Contrera JF, Weaver JL, Willard JM, Hastings KL, Sancilio LF.

Toxicol Mech Methods · journal article · DOI 10.1080/15376510701857262

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 2003-10-01

Identification and prediction of promiscuous aggregating inhibitors among known drugs.

Seidler J, McGovern SL, Doman TN, Shoichet BK.

J Med Chem · research support, u.s. gov't, p.h.s.; research support, non-u.s. gov't; journal article · DOI 10.1021/jm030191r

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Publikationer i urvalet

Discovery of novel pyrrolo[2,1-c][1,4]benzodiazepine-3,11-dione (PBD) derivatives as selective HDAC6 inhibitors for the efficient treatment of idiopathic pulmonary fibrosis (IPF) in vitro and in vivo.

Identification of a Novel Selective CDK9 Inhibitor for the Treatment of CRC: Design, Synthesis, and Biological Activity Evaluation.

Discovery of the First Potent, Selective, and <i>In Vivo</i> Efficacious Polo-like Kinase 4 Proteolysis Targeting Chimera Degrader for the Treatment of <i>TRIM37</i>-Amplified Breast Cancer.

Discovery of CZS-241: A Potent, Selective, and Orally Available Polo-Like Kinase 4 Inhibitor for the Treatment of Chronic Myeloid Leukemia.

Identification of N- and C-3-Modified Laudanosoline Derivatives as Novel Influenza PA<sub>N</sub> Endonuclease Inhibitors.

Structure-based discovery of 1-(3-fluoro-5-(5-(3-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl)phenyl)-3-(pyrimidin-5-yl)urea as a potent and selective nanomolar type-II PLK4 inhibitor.

Design, synthesis, and antibacterial activity of derivatives of Tryptophanyl-tRNA synthetase inhibitor indolmycin.

Discovery of a non-zwitterionic oseltamivir analogue as a potent influenza a neuraminidase inhibitor.

Design, Synthesis, and Mechanism Study of Benzenesulfonamide-Containing Phenylalanine Derivatives as Novel HIV-1 Capsid Inhibitors with Improved Antiviral Activities.

Design, synthesis and structure-activity relationships of 4-phenyl-1H-1,2,3-triazole phenylalanine derivatives as novel HIV-1 capsid inhibitors with promising antiviral activities.

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

Design, synthesis and biological evaluation of oseltamivir derivatives containing pyridyl group as potent inhibitors of neuraminidase for influenza A.

Structure-Based Optimization of N-Substituted Oseltamivir Derivatives as Potent Anti-Influenza A Virus Agents with Significantly Improved Potency against Oseltamivir-Resistant N1-H274Y Variant.

Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.

Structure-based identification of OATP1B1/3 inhibitors.

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

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

Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.

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

Identification and prediction of promiscuous aggregating inhibitors among known drugs.