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Volumn 5, Issue 4, 2014, Pages 378-383

Discovery and optimization of tetramethylpiperidinyl benzamides as inhibitors of EZH2

Author keywords

diphenylether; EZH2; KARPAS 422; methyltransferase; PRC2; tetramethylpiperidine

Indexed keywords

BENZAMIDE DERIVATIVE; EPZ 6438; GSK 126; PROTEIN INHIBITOR; TRANSCRIPTION FACTOR EZH2; TRANSCRIPTION FACTOR EZH2 INHIBITOR; UNC 1999; UNCLASSIFIED DRUG;

EID: 84898034702     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/ml400494b     Document Type: Article
Times cited : (62)

References (25)
  • 1
    • 78751662908 scopus 로고    scopus 로고
    • The Polycomb Complex PRC2 and Its Mark in Life
    • Margueron, R.; Reinberg, D. The Polycomb Complex PRC2 and Its Mark in Life Nature 2011, 469, 343-349
    • (2011) Nature , vol.469 , pp. 343-349
    • Margueron, R.1    Reinberg, D.2
  • 6
    • 78650454078 scopus 로고    scopus 로고
    • Coordinated Activities of Wild-Type Plus Mutant EZH2 Drive Tumor-Associated Hypertrimethylation of Lysine 27 on Histone H3 (H3K27) in Human B-Cell Lymphomas
    • Sneeringer, C. J.; Scott, M. P.; Kuntz, K. W.; Knutson, S. K.; Pollock, R. M.; Richon, V. M.; Copeland, R. A. Coordinated Activities of Wild-Type Plus Mutant EZH2 Drive Tumor-Associated Hypertrimethylation of Lysine 27 on Histone H3 (H3K27) in Human B-Cell Lymphomas Proc. Natl. Acad. Sci. 2010, 107, 20980-20985
    • (2010) Proc. Natl. Acad. Sci. , vol.107 , pp. 20980-20985
    • Sneeringer, C.J.1    Scott, M.P.2    Kuntz, K.W.3    Knutson, S.K.4    Pollock, R.M.5    Richon, V.M.6    Copeland, R.A.7
  • 16
    • 84884135909 scopus 로고    scopus 로고
    • Chapter Thirteen: Recent Advances in Small-Molecule Modulation of Epigenetic Targets: Discovery and Development of Histone Methyltransferase and Bromodomain Inhibitors
    • Sweis, R. F.; Michaelides, M. R. Chapter Thirteen: Recent Advances in Small-Molecule Modulation of Epigenetic Targets: Discovery and Development of Histone Methyltransferase and Bromodomain Inhibitors Annu. Rep. Med. Chem. 2013, 48, 185-203
    • (2013) Annu. Rep. Med. Chem. , vol.48 , pp. 185-203
    • Sweis, R.F.1    Michaelides, M.R.2
  • 18
    • 33845491449 scopus 로고    scopus 로고
    • Interpreting Steep Dose-Response Curves in Early Inhibitor Discovery
    • Shoichet, B. K. Interpreting Steep Dose-Response Curves in Early Inhibitor Discovery J. Med. Chem. 2006, 49, 7274-7277
    • (2006) J. Med. Chem. , vol.49 , pp. 7274-7277
    • Shoichet, B.K.1
  • 20
    • 84885172160 scopus 로고    scopus 로고
    • Improving the Plausibility of Success with Inefficient Metrics
    • Shultz, M. D. Improving the Plausibility of Success with Inefficient Metrics Bioorg. Med. Chem. Lett. 2013, 23, 5980-5991
    • (2013) Bioorg. Med. Chem. Lett. , vol.23 , pp. 5980-5991
    • Shultz, M.D.1
  • 21
    • 84885190072 scopus 로고    scopus 로고
    • The Thermodynamic Basis for the Use of Lipophilic Efficiency (LipE) in Enthalpic Optimizations
    • Shultz, M. D. The Thermodynamic Basis for the Use of Lipophilic Efficiency (LipE) in Enthalpic Optimizations Bioorg. Med. Chem. Lett. 2013, 23, 5992-6000
    • (2013) Bioorg. Med. Chem. Lett. , vol.23 , pp. 5992-6000
    • Shultz, M.D.1
  • 22
    • 0013178339 scopus 로고
    • Absorption Spectra of Some Highly Substituted Diaryl Ethers
    • Dahlgard, M.; Brewster, R. Q. Absorption Spectra of Some Highly Substituted Diaryl Ethers J. Am. Chem. Soc. 1958, 80, 5861-5863
    • (1958) J. Am. Chem. Soc. , vol.80 , pp. 5861-5863
    • Dahlgard, M.1    Brewster, R.Q.2
  • 23
    • 34250247798 scopus 로고
    • Calculation of the Conformation of Diphenylamine and its ortho - And para -Nitro-Derivatives by the Method of Atom-Atom Potentials
    • Gusakova, N. N.; Pankratov, A. N.; Fedorov, E. E.; Mushtakova, S. P.; Gribov, L. A. Calculation of the Conformation of Diphenylamine and its ortho-and para -Nitro-Derivatives by the Method of Atom-Atom Potentials J. Struct. Chem. 1981, 22, 341-345
    • (1981) J. Struct. Chem. , vol.22 , pp. 341-345
    • Gusakova, N.N.1    Pankratov, A.N.2    Fedorov, E.E.3    Mushtakova, S.P.4    Gribov, L.A.5
  • 24
    • 39449105474 scopus 로고    scopus 로고
    • Small Molecule Conformational Preferences Derived from Crystal Structure Data. A Medicinal Chemistry Focused Analysis
    • Brameld, K. A.; Kuhn, B.; Reuter, D. C.; Stahl, M. Small Molecule Conformational Preferences Derived from Crystal Structure Data. A Medicinal Chemistry Focused Analysis J. Chem. Inf. Model. 2008, 48, 1-24
    • (2008) J. Chem. Inf. Model. , vol.48 , pp. 1-24
    • Brameld, K.A.1    Kuhn, B.2    Reuter, D.C.3    Stahl, M.4


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.