메뉴 건너뛰기




Volumn 56, Issue 5, 2013, Pages 1878-1893

Optimized S-trityl-l-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models

Author keywords

[No Author keywords available]

Indexed keywords

2 AMINO 3 (((3 ETHYL 4 METHYLPHENYL)(DIPHENYL)METHYL)SULFANYL)PROPANOIC ACID; 2 AMINO 5 (3,4 DIMETHYLPHENYL) 5,5 DIPHENYLPENTANOIC ACID; ANTINEOPLASTIC AGENT; CYTOCHROME P450; ISPINESIB; KINESIN; PHENYL GROUP; POTASSIUM CHANNEL HERG; PROPIONIC ACID; S TRITYL LEVO CYSTEINE; SB 743921; UNCLASSIFIED DRUG; VALERIC ACID;

EID: 84875204980     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm3014597     Document Type: Article
Times cited : (41)

References (76)
  • 2
    • 70349437416 scopus 로고    scopus 로고
    • Kinesin superfamily motor proteins and intracellular transport
    • Hirokawa, N.; Noda, Y.; Tanaka, Y.; Niwa, S. Kinesin superfamily motor proteins and intracellular transport Nat. Rev. Mol. Cell Biol. 2009, 10, 682-696
    • (2009) Nat. Rev. Mol. Cell Biol. , vol.10 , pp. 682-696
    • Hirokawa, N.1    Noda, Y.2    Tanaka, Y.3    Niwa, S.4
  • 3
    • 82755185858 scopus 로고    scopus 로고
    • Elucidating the functionality of kinesins: An overview of small molecule inhibitors
    • Good, J. A. D.; Skoufias, D. A.; Kozielski, F. Elucidating the functionality of kinesins: An overview of small molecule inhibitors Semin. Cell Dev. Biol. 2011, 22, 935-945
    • (2011) Semin. Cell Dev. Biol. , vol.22 , pp. 935-945
    • Good, J.A.D.1    Skoufias, D.A.2    Kozielski, F.3
  • 4
    • 0026739078 scopus 로고
    • Mitotic spindle organization by a plus-end-directed microtubule motor
    • Sawin, K. E.; LeGuellec, K.; Philippe, M.; Mitchison, T. J. Mitotic spindle organization by a plus-end-directed microtubule motor Nature 1992, 359, 540-543
    • (1992) Nature , vol.359 , pp. 540-543
    • Sawin, K.E.1    Leguellec, K.2    Philippe, M.3    Mitchison, T.J.4
  • 5
    • 0029417238 scopus 로고
    • Phosphorylation by p34cdc2 regulates spindle association of human Eg5, a kinesin-related motor essential for bipolar spindle formation in vivo
    • Blangy, A.; Lane, H. A.; d'Hérin, P.; Harper, M.; Kress, M.; Nigg, E. A. Phosphorylation by p34cdc2 regulates spindle association of human Eg5, a kinesin-related motor essential for bipolar spindle formation in vivo Cell 1995, 83, 1159-1169
    • (1995) Cell , vol.83 , pp. 1159-1169
    • Blangy, A.1    Lane, H.A.2    D'Hérin, P.3    Harper, M.4    Kress, M.5    Nigg, E.A.6
  • 6
    • 0033615357 scopus 로고    scopus 로고
    • Small Molecule Inhibitor of Mitotic Spindle Bipolarity Identified in a Phenotype-Based Screen
    • Mayer, T. U.; Kapoor, T. M.; Haggarty, S. J.; King, R. W.; Schreiber, S. L.; Mitchison, T. J. Small Molecule Inhibitor of Mitotic Spindle Bipolarity Identified in a Phenotype-Based Screen Science 1999, 286, 971-974
    • (1999) Science , vol.286 , pp. 971-974
    • Mayer, T.U.1    Kapoor, T.M.2    Haggarty, S.J.3    King, R.W.4    Schreiber, S.L.5    Mitchison, T.J.6
  • 10
    • 47249083435 scopus 로고    scopus 로고
    • Recent progress in the identification and clinical evaluation of inhibitors of the mitotic kinesin KSP
    • DOI 10.2174/156802608784911626
    • Knight, S. D.; Parrish, C. A. Recent Progress in the Identification and Clinical Evaluation of Inhibitors of the Mitotic Kinesin KSP Curr. Topics Med. Chem. 2008, 8, 888-904 (Pubitemid 351984711)
    • (2008) Current Topics in Medicinal Chemistry , vol.8 , Issue.10 , pp. 888-904
    • Knight, S.D.1    Parrish, C.A.2
  • 13
    • 0035816597 scopus 로고    scopus 로고
    • Crystal Structure of the Mitotic Spindle Kinesin Eg5 Reveals a Novel Conformation of the Neck-linker
    • Turner, J.; Anderson, R.; Guo, J.; Beraud, C.; Fletterick, R.; Sakowicz, R. Crystal Structure of the Mitotic Spindle Kinesin Eg5 Reveals a Novel Conformation of the Neck-linker J. Biol. Chem. 2001, 276, 25496-25502
    • (2001) J. Biol. Chem. , vol.276 , pp. 25496-25502
    • Turner, J.1    Anderson, R.2    Guo, J.3    Beraud, C.4    Fletterick, R.5    Sakowicz, R.6
  • 14
    • 84859783708 scopus 로고    scopus 로고
    • A Phase I/II Trial of the Kinesin Spindle Protein (KSP) Inhibitor SB-743921 Dosed Q14D without and with Prophylactic G-CSF in Non-Hodgkin (NHL) or Hodgkin Lymphoma (HL)
    • O'Connor, O. A.; Gerecitano, J.; Van Deventer, H.; Afanasyev, B.; Hainsworth, J.; Chen, M.; Saikali, K.; Seroogy, J.; Escandon, R.; Wolff, A.; Conlan, M. G. A Phase I/II Trial of the Kinesin Spindle Protein (KSP) Inhibitor SB-743921 Dosed Q14D without and with Prophylactic G-CSF in Non-Hodgkin (NHL) or Hodgkin Lymphoma (HL) Blood 2009, 114, 667-667
    • (2009) Blood , vol.114 , pp. 667-667
    • O'Connor, O.A.1    Gerecitano, J.2    Van Deventer, H.3    Afanasyev, B.4    Hainsworth, J.5    Chen, M.6    Saikali, K.7    Seroogy, J.8    Escandon, R.9    Wolff, A.10    Conlan, M.G.11
  • 16
    • 84875186486 scopus 로고    scopus 로고
    • Combination of the KSP Inhibitor ARRY-520 with Bortezomib or Revlimid Causes Sustained Tumor Regressions and Significantly Increased Time to Regrowth in Models of Multiple Myeloma
    • Woessner, R.; Tunquist, B.; Cox, A.; Rana, S.; Walker, D.; Lee, P. A. Combination of the KSP Inhibitor ARRY-520 with Bortezomib or Revlimid Causes Sustained Tumor Regressions and Significantly Increased Time to Regrowth in Models of Multiple Myeloma Blood 2009, 114, 1115-1116
    • (2009) Blood , vol.114 , pp. 1115-1116
    • Woessner, R.1    Tunquist, B.2    Cox, A.3    Rana, S.4    Walker, D.5    Lee, P.A.6
  • 18
    • 33745867225 scopus 로고    scopus 로고
    • S-trityl-L-cysteine is a reversible, tight binding inhibitor of the human kinesin Eg5 that specifically blocks mitotic progression
    • DOI 10.1074/jbc.M511735200
    • Skoufias, D. A.; DeBonis, S.; Saoudi, Y.; Lebeau, L.; Crevel, I.; Cross, R.; Wade, R. H.; Hackney, D.; Kozielski, F. S -Trityl- l -cysteine Is a Reversible, Tight Binding Inhibitor of the Human Kinesin Eg5 That Specifically Blocks Mitotic Progression J. Biol. Chem. 2006, 281, 17559-17569 (Pubitemid 44035555)
    • (2006) Journal of Biological Chemistry , vol.281 , Issue.26 , pp. 17559-17569
    • Skoufias, D.A.1    DeBonis, S.2    Saoudi, Y.3    Lebeau, L.4    Crevel, I.5    Cross, R.6    Wade, R.H.7    Hackney, D.8    Kozielski, F.9
  • 19
    • 5444274954 scopus 로고    scopus 로고
    • Identification of the protein binding region of S-trityl-L-cysteine, a new potent inhibitor of the mitotic kinesin Eg5
    • DOI 10.1021/bi049264e
    • Brier, S.; Lemaire, D.; DeBonis, S.; Forest, E.; Kozielski, F. Identification of the Protein Binding Region of S -Trityl- l -cysteine, a New Potent Inhibitor of the Mitotic Kinesin Eg5 Biochemistry 2004, 43, 13072-13082 (Pubitemid 39362777)
    • (2004) Biochemistry , vol.43 , Issue.41 , pp. 13072-13082
    • Brier, S.1    Lemaire, D.2    DeBonis, S.3    Forest, E.4    Kozielski, F.5
  • 20
    • 38949179546 scopus 로고    scopus 로고
    • Proteome analysis of apoptosis signaling by S-trityl-L-cysteine, a potent reversible inhibitor of human mitotic kinesin Eg5
    • DOI 10.1002/pmic.200700534
    • Kozielski, F.; Skoufias, D. A.; Indorato, R.-L.; Saoudi, Y.; Jungblut, P. R.; Hustoft, H. K.; Strozynski, M.; Thiede, B. Proteome analysis of apoptosis signaling by S -trityl- l -cysteine, a potent reversible inhibitor of human mitotic kinesin Eg5 Proteomics 2008, 8, 289-300 (Pubitemid 351212328)
    • (2008) Proteomics , vol.8 , Issue.2 , pp. 289-300
    • Kozielski, F.1    Skoufias, D.A.2    Indorato, R.-L.3    Saoudi, Y.4    Jungblut, P.R.5    Hustoff, H.K.6    Strozynski, M.7    Thiede, B.8
  • 21
    • 0014785803 scopus 로고
    • Experimental antileukemic agents. Preparation and structure-activity study of S -tritylcysteine and related compounds
    • Zee-Cheng, K.-Y.; Cheng, C.-C. Experimental antileukemic agents. Preparation and structure-activity study of S -tritylcysteine and related compounds J. Med. Chem. 1970, 13, 414-418
    • (1970) J. Med. Chem. , vol.13 , pp. 414-418
    • Zee-Cheng, K.-Y.1    Cheng, C.-C.2
  • 22
    • 77956636408 scopus 로고    scopus 로고
    • A Potent Chemotherapeutic Strategy for Bladder Cancer: (S)-Methoxy-Trityl-L-Cystein, a Novel Eg5 Inhibitor
    • Ding, S.; Nishizawa, K.; Kobayashi, T.; Oishi, S.; Lv, J.; Fujii, N.; Ogawa, O.; Nishiyama, H. A Potent Chemotherapeutic Strategy for Bladder Cancer: (S)-Methoxy-Trityl-L-Cystein, a Novel Eg5 Inhibitor J. Urol. 2010, 184, 1175-1181
    • (2010) J. Urol. , vol.184 , pp. 1175-1181
    • Ding, S.1    Nishizawa, K.2    Kobayashi, T.3    Oishi, S.4    Lv, J.5    Fujii, N.6    Ogawa, O.7    Nishiyama, H.8
  • 25
    • 34250328223 scopus 로고    scopus 로고
    • Synthesis and biological evaluation of l-cysteine derivatives as mitotic kinesin Eg5 inhibitors
    • DOI 10.1016/j.bmcl.2007.04.101, PII S0960894X07005318
    • Ogo, N.; Oishi, S.; Matsuno, K.; Sawada, J.-i.; Fujii, N.; Asai, A. Synthesis and biological evaluation of l -cysteine derivatives as mitotic kinesin Eg5 inhibitors Bioorg. Med. Chem. Lett. 2007, 17, 3921-3924 (Pubitemid 46920939)
    • (2007) Bioorganic and Medicinal Chemistry Letters , vol.17 , Issue.14 , pp. 3921-3924
    • Ogo, N.1    Oishi, S.2    Matsuno, K.3    Sawada, J.-i.4    Fujii, N.5    Asai, A.6
  • 26
    • 79952778930 scopus 로고    scopus 로고
    • Structure-Activity Relationship and Multidrug Resistance Study of New S -trityl- l -Cysteine Derivatives As Inhibitors of Eg5
    • Kaan, H. Y. K.; Weiss, J.; Menger, D.; Ulaganathan, V.; Tkocz, K.; Laggner, C.; Popowycz, F.; Joseph, B.; Kozielski, F. Structure-Activity Relationship and Multidrug Resistance Study of New S -trityl- l -Cysteine Derivatives As Inhibitors of Eg5 J. Med. Chem. 2011, 54, 1576-1586
    • (2011) J. Med. Chem. , vol.54 , pp. 1576-1586
    • Kaan, H.Y.K.1    Weiss, J.2    Menger, D.3    Ulaganathan, V.4    Tkocz, K.5    Laggner, C.6    Popowycz, F.7    Joseph, B.8    Kozielski, F.9
  • 27
    • 72449183762 scopus 로고    scopus 로고
    • An allosteric transition trapped in an intermediate state of a new kinesin-inhibitor complex
    • Kaan, H. Y. K.; Ulaganathan, V.; Hackney, D. D.; Kozielski, F. An allosteric transition trapped in an intermediate state of a new kinesin-inhibitor complex Biochem. J. 2010, 425, 55-60
    • (2010) Biochem. J. , vol.425 , pp. 55-60
    • Kaan, H.Y.K.1    Ulaganathan, V.2    Hackney, D.D.3    Kozielski, F.4
  • 31
    • 0035900353 scopus 로고    scopus 로고
    • Reductive demercuration in deprotection of trityl thioethers, trityl amines, and trityl ethers
    • DOI 10.1021/jo0156971
    • Maltese, M. Reductive Demercuration in Deprotection of Trityl Thioethers, Trityl Amines, and Trityl Ethers J. Org. Chem. 2001, 66, 7615-7625 (Pubitemid 33063953)
    • (2001) Journal of Organic Chemistry , vol.66 , Issue.23 , pp. 7615-7625
    • Maltese, M.1
  • 32
    • 27844466269 scopus 로고
    • N -methoxy- N -methylamides as effective acylating agents
    • Nahm, S.; Weinreb, S. M. N -methoxy- N -methylamides as effective acylating agents Tetrahedron Lett. 1981, 22, 3815-3818
    • (1981) Tetrahedron Lett. , vol.22 , pp. 3815-3818
    • Nahm, S.1    Weinreb, S.M.2
  • 33
    • 34548158464 scopus 로고    scopus 로고
    • Iron trichloride mediated allylation of lithium alkoxides through an unusual carbon-oxygen bond cleavage
    • DOI 10.1021/om700522q
    • Kabalka, G. W.; Yao, M.-L.; Borella, S.; Goins, L. K. Iron Trichloride Mediated Allylation of Lithium Alkoxides through an Unusual Carbon-Oxygen Bond Cleavage Organometallics 2007, 26, 4112-4114 (Pubitemid 47310039)
    • (2007) Organometallics , vol.26 , Issue.17 , pp. 4112-4114
    • Kabalka, G.W.1    Yao, M.-L.2    Borella, S.3    Goins, L.K.4
  • 34
    • 33644528891 scopus 로고
    • Readily accessible 12-I-5 oxidant for the conversion of primary and secondary alcohols to aldehydes and ketones
    • Dess, D. B.; Martin, J. C. Readily accessible 12-I-5 oxidant for the conversion of primary and secondary alcohols to aldehydes and ketones J. Org. Chem. 1983, 48, 4155-4156
    • (1983) J. Org. Chem. , vol.48 , pp. 4155-4156
    • Dess, D.B.1    Martin, J.C.2
  • 35
    • 0842311253 scopus 로고    scopus 로고
    • Montmorillonite KSF clay catalyzed one-pot synthesis of α-aminonitriles
    • DOI 10.1016/j.tet.2003.12.043
    • Yadav, J. S.; Reddy, B. V. S.; Eeshwaraiah, B.; Srinivas, M. Montmorillonite KSF clay catalyzed one-pot synthesis of α-aminonitriles Tetrahedron 2004, 60, 1767-1771 (Pubitemid 38183066)
    • (2004) Tetrahedron , vol.60 , Issue.8 , pp. 1767-1771
    • Yadav, J.S.1    Subba Reddy, B.V.2    Eeshwaraiah, B.3    Srinivas, M.4
  • 36
    • 84948302995 scopus 로고
    • Debenzylation of N -Benzylamino Derivatives by Catalytic Transfer Hydrogenation with Ammonium Formate
    • Ram, S.; Spicer, L. D. Debenzylation of N -Benzylamino Derivatives by Catalytic Transfer Hydrogenation With Ammonium Formate Synth. Commun. 1987, 17, 415-418
    • (1987) Synth. Commun. , vol.17 , pp. 415-418
    • Ram, S.1    Spicer, L.D.2
  • 37
    • 0001755016 scopus 로고    scopus 로고
    • Nonracemic α-Fluoro Aldehydes: Asymmetric Synthesis of 4-Deoxy-4-fluoro-D-arabinopyranose
    • Davis, F. A.; Kasu, P. V. N.; Sundarababu, G.; Qi, H. Nonracemic α-Fluoro Aldehydes: Asymmetric Synthesis of 4-Deoxy-4-fluoro- d -arabinopyranose J. Org. Chem. 1997, 62, 7546-7547 (Pubitemid 127494393)
    • (1997) Journal of Organic Chemistry , vol.62 , Issue.22 , pp. 7546-7547
    • Davis, F.A.1    Kasu, P.V.N.2    Sundarababu, G.3    Qi, H.4
  • 38
    • 20944444147 scopus 로고    scopus 로고
    • Enantioselective Organocatalytic α-Fluorination of Aldehydes
    • Beeson, T. D.; MacMillan, D. W. C. Enantioselective Organocatalytic α-Fluorination of Aldehydes J. Am. Chem. Soc. 2005, 127, 8826-8828
    • (2005) J. Am. Chem. Soc. , vol.127 , pp. 8826-8828
    • Beeson, T.D.1    MacMillan, D.W.C.2
  • 39
    • 17144415210 scopus 로고    scopus 로고
    • Direct Organocatalytic α-Fluorination of Aldehydes and Ketones
    • Enders, D.; Hüttl, M. R. M. Direct Organocatalytic α-Fluorination of Aldehydes and Ketones Synlett 2005, 2005, 0991-0993
    • (2005) Synlett , vol.2005 , pp. 0991-0993
    • Enders, D.1    Hüttl, M.R.M.2
  • 41
    • 3543029840 scopus 로고    scopus 로고
    • Regioselective and stereoselective nucleophilic ring opening of trifluoromethylated cyclic sulfates: Asymmetric synthesis of both enantiomers of syn-(3-trifluoromethyl)isoserine
    • DOI 10.1021/jo0497611
    • Jiang, Z.-X.; Qing, F.-L. Regioselective and Stereoselective Nucleophilic Ring Opening of Trifluoromethylated Cyclic Sulfates: Asymmetric Synthesis of Both Enantiomers of syn -(3-Trifluoromethyl)isoserine J. Org. Chem. 2004, 69, 5486-5489 (Pubitemid 39014389)
    • (2004) Journal of Organic Chemistry , vol.69 , Issue.16 , pp. 5486-5489
    • Jiang, Z.-X.1    Qing, F.-L.2
  • 42
    • 77956918409 scopus 로고    scopus 로고
    • S -trityl- l -cysteine derivative induces caspase-independent cell death in K562 human chronic myeloid leukemia cell line
    • Shimizu, M.; Ishii, H.; Ogo, N.; Unno, Y.; Matsuno, K.; Sawada, J.-i.; Akiyama, Y.; Asai, A. S -trityl- l -cysteine derivative induces caspase-independent cell death in K562 human chronic myeloid leukemia cell line Cancer Lett. 2010, 298, 99-106
    • (2010) Cancer Lett. , vol.298 , pp. 99-106
    • Shimizu, M.1    Ishii, H.2    Ogo, N.3    Unno, Y.4    Matsuno, K.5    Sawada, J.-I.6    Akiyama, Y.7    Asai, A.8
  • 43
    • 33749626306 scopus 로고    scopus 로고
    • Regulation and targeting of Eg5, a mitotic motor protein in blast crisis CML: Overcoming imatinib resistance
    • Carter, B. Z.; Mak, D. H.; Shi, Y.; Schober, W. D.; Wang, R.-Y.; Konopleva, M.; Koller, E.; Dean, N. M.; Andreeff, M. Regulation and Targeting of Eg5, a Mitotic Motor Protein in Blast Crisis CML: Overcoming Imatinib Resistance Cell Cycle 2006, 5, 2223-2229 (Pubitemid 44546558)
    • (2006) Cell Cycle , vol.5 , Issue.19 , pp. 2223-2229
    • Carter, B.Z.1    Mak, D.H.2    Shi, Y.3    Schober, W.D.4    Wang, R.-Y.5    Konopleva, M.6    Koller, E.7    Dean, N.M.8    Andreeff, M.9
  • 45
    • 0030592950 scopus 로고    scopus 로고
    • Characterisation of the toxic metabolite(s) of naphthalene
    • DOI 10.1016/S0300-483X(96)03515-9, PII S0300483X96035159
    • Wilson, A. S.; Davis, C. D.; Williams, D. P.; Buckpitt, A. R.; Pirmohamed, M.; Park, B. K. Characterisation of the toxic metabolite(s) of naphthalene Toxicology 1996, 114, 233-242 (Pubitemid 26421936)
    • (1996) Toxicology , vol.114 , Issue.3 , pp. 233-242
    • Wilson, A.S.1    Davis, C.D.2    Williams, D.P.3    Buckpitt, A.R.4    Pirmohamed, M.5    Park, B.K.6
  • 46
    • 28544448146 scopus 로고
    • Incorporation of Radioactive L-Cystine by Normal and Leukemic Leukocytes in Vivo
    • Weisberger, A. S.; Levine, B. Incorporation of Radioactive L-Cystine by Normal and Leukemic Leukocytes in Vivo Blood 1954, 9, 1082-1094
    • (1954) Blood , vol.9 , pp. 1082-1094
    • Weisberger, A.S.1    Levine, B.2
  • 47
    • 0012359979 scopus 로고
    • Potential Anticancer Agents. V. Some Sulfur-Substituted Derivatives of Cysteine
    • Goodman, L.; Ross, L. O.; Baker, B. R. Potential Anticancer Agents. V. Some Sulfur-Substituted Derivatives of Cysteine J. Org. Chem. 1958, 23, 1251-1257
    • (1958) J. Org. Chem. , vol.23 , pp. 1251-1257
    • Goodman, L.1    Ross, L.O.2    Baker, B.R.3
  • 48
    • 77749315417 scopus 로고    scopus 로고
    • Lipophilicity in drug discovery
    • Waring, M. J. Lipophilicity in drug discovery Expert Opin. Drug Discovery 2010, 5, 235-248
    • (2010) Expert Opin. Drug Discovery , vol.5 , pp. 235-248
    • Waring, M.J.1
  • 52
    • 77955386873 scopus 로고    scopus 로고
    • Structural Basis for Inhibition of Eg5 by Dihydropyrimidines: Stereoselectivity of Antimitotic Inhibitors Enastron, Dimethylenastron, and Fluorastrol
    • Kaan, H. Y. K.; Ulaganathan, V.; Rath, O.; Prokopcová, H.; Dallinger, D.; Kappe, C. O.; Kozielski, F. Structural Basis for Inhibition of Eg5 by Dihydropyrimidines: Stereoselectivity of Antimitotic Inhibitors Enastron, Dimethylenastron, and Fluorastrol J. Med. Chem. 2010, 53, 5676-5683
    • (2010) J. Med. Chem. , vol.53 , pp. 5676-5683
    • Kaan, H.Y.K.1    Ulaganathan, V.2    Rath, O.3    Prokopcová, H.4    Dallinger, D.5    Kappe, C.O.6    Kozielski, F.7
  • 54
    • 27644596457 scopus 로고    scopus 로고
    • Predicting in vivo drug interactions from in vitro drug discovery data
    • DOI 10.1038/nrd1851, PII N1851
    • Wienkers, L. C.; Heath, T. G. Predicting in vivo drug interactions from in vitro drug discovery data Nat. Rev. Drug Discovery 2005, 4, 825-833 (Pubitemid 41553963)
    • (2005) Nature Reviews Drug Discovery , vol.4 , Issue.10 , pp. 825-833
    • Wienkers, L.C.1    Heath, T.G.2
  • 55
    • 33747505446 scopus 로고    scopus 로고
    • Medicinal chemistry of hERG optimizations: Highlights and hang-ups
    • DOI 10.1021/jm060379l
    • Jamieson, C.; Moir, E. M.; Rankovic, Z.; Wishart, G. Medicinal Chemistry of hERG Optimizations: Highlights and Hang-Ups J. Med. Chem. 2006, 49, 5029-5046 (Pubitemid 44260200)
    • (2006) Journal of Medicinal Chemistry , vol.49 , Issue.17 , pp. 5029-5046
    • Jamieson, C.1    Moir, E.M.2    Rankovic, Z.3    Wishart, G.4
  • 57
    • 52449105346 scopus 로고    scopus 로고
    • Survival from lung cancer in England and Wales up to 2001
    • Zee, Y. K.; Eisen, T. Survival from lung cancer in England and Wales up to 2001 Br. J. Cancer 2008, 99, S43-S46
    • (2008) Br. J. Cancer , vol.99
    • Zee, Y.K.1    Eisen, T.2
  • 58
    • 2042422004 scopus 로고    scopus 로고
    • Human tumor xenografts. Predictivity, characterization and discovery of new new anticancer agents
    • In; Fiebig, H. H. Burger, A. M. Karger: Basel, Vol.
    • Fiebig, H. H.; Dengler, W. A.; Roth, T. Human tumor xenografts. Predictivity, characterization and discovery of new new anticancer agents. In Relevance of tumor models for anticancer drug development; Fiebig, H. H.; Burger, A. M., Eds.; Karger: Basel, 1999; Vol. 54, pp 29-50.
    • (1999) Relevance of Tumor Models for Anticancer Drug Development , vol.54 , pp. 29-50
    • Fiebig, H.H.1    Dengler, W.A.2    Roth, T.3
  • 61
    • 84855431740 scopus 로고    scopus 로고
    • Inhibitors Targeting Mitosis: Tales of How Great Drugs against a Promising Target Were Brought Down by a Flawed Rationale
    • Komlodi-Pasztor, E.; Sackett, D. L.; Fojo, A. T. Inhibitors Targeting Mitosis: Tales of How Great Drugs against a Promising Target Were Brought Down by a Flawed Rationale Clin. Cancer Res. 2012, 18, 51-63
    • (2012) Clin. Cancer Res. , vol.18 , pp. 51-63
    • Komlodi-Pasztor, E.1    Sackett, D.L.2    Fojo, A.T.3
  • 63
    • 33746700189 scopus 로고    scopus 로고
    • Benzimidazole derivatives bearing substituted biphenyls as hepatitis C virus NS5B RNA-dependent RNA polymerase inhibitors: Structure-activity relationship studies and identification of a potent and highly selective inhibitor JTK-109
    • DOI 10.1021/jm060269e
    • Hirashima, S.; Suzuki, T.; Ishida, T.; Noji, S.; Yata, S.; Ando, I.; Komatsu, M.; Ikeda, S.; Hashimoto, H. Benzimidazole Derivatives Bearing Substituted Biphenyls as Hepatitis C Virus NS5B RNA-Dependent RNA Polymerase Inhibitors: Structure-Activity Relationship Studies and Identification of a Potent and Highly Selective Inhibitor JTK-109 J. Med. Chem. 2006, 49, 4721-4736 (Pubitemid 44162700)
    • (2006) Journal of Medicinal Chemistry , vol.49 , Issue.15 , pp. 4721-4736
    • Hirashima, S.1    Suzuki, T.2    Ishida, T.3    Noji, S.4    Yata, S.5    Ando, I.6    Komatsu, M.7    Ikeda, S.8    Hashimoto, H.9
  • 64
    • 33749257679 scopus 로고    scopus 로고
    • Dicationic DNA-targeted antiprotozoal agents: Naphthalene replacement of benzimidazole
    • DOI 10.1016/j.bmc.2006.07.024, PII S0968089606005773
    • Chackal-Catoen, S.; Miao, Y.; Wilson, W. D.; Wenzler, T.; Brun, R.; Boykin, D. W. Dicationic DNA-targeted antiprotozoal agents: Naphthalene replacement of benzimidazole Bioorg. Med. Chem. 2006, 14, 7434-7445 (Pubitemid 44486805)
    • (2006) Bioorganic and Medicinal Chemistry , vol.14 , Issue.22 , pp. 7434-7445
    • Chackal-Catoen, S.1    Miao, Y.2    Wilson, W.D.3    Wenzler, T.4    Brun, R.5    Boykin, D.W.6
  • 65
    • 10044264293 scopus 로고    scopus 로고
    • Mechanism of inhibition of human KSP by monastrol: Insights from kinetic analysis and the effect of ionic strength on KSP inhibition
    • DOI 10.1021/bi048282t
    • Luo, L.; Carson, J. D.; Dhanak, D.; Jackson, J. R.; Huang, P. S.; Lee, Y.; Sakowicz, R.; Copeland, R. A. Mechanism of Inhibition of Human KSP by Monastrol: Insights from Kinetic Analysis and the Effect of Ionic Strength on KSP Inhibition Biochemistry 2004, 43, 15258-15266 (Pubitemid 39602187)
    • (2004) Biochemistry , vol.43 , Issue.48 , pp. 15258-15266
    • Luo, L.1    Carson, J.D.2    Dhanak, D.3    Jackson, J.R.4    Huang, P.S.5    Lee, Y.6    Sakowicz, R.7    Copeland, R.A.8
  • 66
    • 0014454095 scopus 로고
    • Kinetics of the reversible inhibition of enzyme-catalysed reactions by tight-binding inhibitors
    • Morrison, J. F. Kinetics of the reversible inhibition of enzyme-catalysed reactions by tight-binding inhibitors Biochim. Biophys. Acta, Enzymol. 1969, 185, 269-286
    • (1969) Biochim. Biophys. Acta, Enzymol. , vol.185 , pp. 269-286
    • Morrison, J.F.1
  • 67
    • 1942453243 scopus 로고    scopus 로고
    • Ligand efficiency: A useful metric for lead selection
    • DOI 10.1016/S1359-6446(04)03069-7, PII S1359644604030697
    • Hopkins, A. L.; Groom, C. R.; Alex, A. Ligand efficiency: a useful metric for lead selection Drug Discovery Today 2004, 9, 430-431 (Pubitemid 38510559)
    • (2004) Drug Discovery Today , vol.9 , Issue.10 , pp. 430-431
    • Hopkins, A.L.1    Groom, C.R.2    Alex, A.3
  • 68
  • 70
    • 0028103275 scopus 로고
    • Collaborative. The CCP4 suite: programs for protein crystallography.
    • Collaborative. The CCP4 suite: programs for protein crystallography. Acta Crystallogr., Sect. D: Biol. Crystallogr. 1994, 50, 760-763.
    • (1994) Acta Crystallogr., Sect. D: Biol. Crystallogr. , vol.50 , pp. 760-763


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.