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Volumn 49, Issue 7, 2006, Pages 2143-2146

Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol- 5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor

Author keywords

[No Author keywords available]

Indexed keywords

1 [4 (4 FLUORO 2 METHYL 1H INDOL 5 YLOXY) 5 METHYLPYRROLO[2,1 F][1,2,4]TRIAZIN 6 YLOXY]PROPAN 2 OL; ALANINE; ALKYL GROUP; BMS 540215; BMS 582664; FUNCTIONAL GROUP; METHYL GROUP; PRODRUG; PROTEIN TYROSINE KINASE INHIBITOR; TRIAZINE DERIVATIVE; UNCLASSIFIED DRUG; VASCULOTROPIN RECEPTOR 2;

EID: 33645670595     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm051106d     Document Type: Article
Times cited : (141)

References (20)
  • 1
    • 0028929803 scopus 로고
    • Angiogenesis in cancer, vascular, rheumatoid and other diseases
    • (a) Folkman, J. Angiogenesis in cancer, vascular, rheumatoid and other diseases. Nat. Med. 1995, 1, 27-31.
    • (1995) Nat. Med. , vol.1 , pp. 27-31
    • Folkman, J.1
  • 2
    • 0034648765 scopus 로고    scopus 로고
    • Angiogenesis in cancer and other diseases
    • (b) Carmeliet, P.; Jain, R. K. Angiogenesis in cancer and other diseases. Nature 2000, 407, 249-257.
    • (2000) Nature , vol.407 , pp. 249-257
    • Carmeliet, P.1    Jain, R.K.2
  • 3
    • 0037399412 scopus 로고    scopus 로고
    • Tyrosine kinases as targets in cancer therapy - Successes and failures
    • Traxler, P. Tyrosine kinases as targets in cancer therapy - successes and failures. Exp. Opin. Ther. Targets 2003, 7, 215.
    • (2003) Exp. Opin. Ther. Targets , vol.7 , pp. 215
    • Traxler, P.1
  • 6
    • 0036796466 scopus 로고    scopus 로고
    • Antiangiogenic agents targeting vascular endothelial growth factor and its receptors in clinical development
    • (a) Sepp-Lorenzino, L.; Thomas, K. A. Antiangiogenic agents targeting vascular endothelial growth factor and its receptors in clinical development. Exp. Opin. Investig. Drugs 2002, 11, 1447-1465.
    • (2002) Exp. Opin. Investig. Drugs , vol.11 , pp. 1447-1465
    • Sepp-Lorenzino, L.1    Thomas, K.A.2
  • 7
    • 0036269854 scopus 로고    scopus 로고
    • Kinase insert domain-containing receptor kinase inhibitors as antiangiogenic agents
    • (b) Bilodeau, M. T.; Fraley, M. E.; Hartman, G. D. Kinase insert domain-containing receptor kinase inhibitors as antiangiogenic agents. Exp. Opin. Invest. Drugs 2002, 11, 737-745.
    • (2002) Exp. Opin. Invest. Drugs , vol.11 , pp. 737-745
    • Bilodeau, M.T.1    Fraley, M.E.2    Hartman, G.D.3
  • 8
    • 1642295074 scopus 로고    scopus 로고
    • Development of vascular endothelial growth factor receptor (VEGFR) kinase inhibitors as antiangiogenic agents in cancer therapy
    • (c) Underiner, T. L.; Ruggeri, B.; Gingrich, D. E. Development of vascular endothelial growth factor receptor (VEGFR) kinase inhibitors as antiangiogenic agents in cancer therapy. Curr. Med. Chem. 2004, 11, 731-745.
    • (2004) Curr. Med. Chem. , vol.11 , pp. 731-745
    • Underiner, T.L.1    Ruggeri, B.2    Gingrich, D.E.3
  • 11
    • 2442669093 scopus 로고    scopus 로고
    • Preclinical evaluation of the tyrosine kinase inhibitor SU11248 as a single agent and in combination with "standard of care" therapeutic agents for the treatment of breast cancer
    • (b) Abrams, T. J.; Murray, L. J.; Pesenti, E.; Walker Holway, V.; Colombo, T.; Lee, L. B.; Cherrington, J. M.; Pryer, N. K. Preclinical evaluation of the tyrosine kinase inhibitor SU11248 as a single agent and in combination with "standard of care" therapeutic agents for the treatment of breast cancer. Mol. Cancer Ther. 2003, 2, 1011-1021.
    • (2003) Mol. Cancer Ther. , vol.2 , pp. 1011-1021
    • Abrams, T.J.1    Murray, L.J.2    Pesenti, E.3    Walker Holway, V.4    Colombo, T.5    Lee, L.B.6    Cherrington, J.M.7    Pryer, N.K.8
  • 12
    • 0037075812 scopus 로고    scopus 로고
    • Novel 4-anilinoquinazolines with C-7 basic side chains: Design and structure activity relationship of a series of potent, orally active, VEGF receptor tyrosine kinase inhibitors
    • (c) Hennequin, L. F.; Stokes, E. S. E.; Thomas, A. P.; Johnstone, C.; Plé, P. A.; Ogilvie, D. J.; Dukes, M.; Wedge, S. R.; Kendrew, J.; Curwen, J. O. Novel 4-anilinoquinazolines with C-7 basic side chains: design and structure activity relationship of a series of potent, orally active, VEGF receptor tyrosine kinase inhibitors. J. Med. Chem. 2002, 45, 1300-1312.
    • (2002) J. Med. Chem. , vol.45 , pp. 1300-1312
    • Hennequin, L.F.1    Stokes, E.S.E.2    Thomas, A.P.3    Johnstone, C.4    Plé, P.A.5    Ogilvie, D.J.6    Dukes, M.7    Wedge, S.R.8    Kendrew, J.9    Curwen, J.O.10
  • 14
    • 10744227153 scopus 로고    scopus 로고
    • A new class of potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: Structure-activity relationships for a series of 9-alkoxymethyl-12-(3-hydroxypropyl)-indeno[2,1-a]pyrrolo[3,4-i-] carbazole-5-ones and the identification of CEP-5214 and its dimethylglycine ester prodrug clinical candidate CEP-7055
    • (e) Gingrich, D. E.; Reddy, D. R.; Iqbal, M. A.; Singh, J.; Aimone, L. D.; Angeles, T. S.; Albom, M.; Yang, S.; Ator, M. A.; Meyer, S. L.; Robinson, C.; Ruggeri, B. A.; Dionne, C. A.; Vaught, J. L.; Mallamo, J. P.; Hudkins, R. L. A new class of potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: structure-activity relationships for a series of 9-alkoxymethyl-12-(3-hydroxypropyl)-indeno[2,1-a]pyrrolo[3,4-i-] carbazole-5-ones and the identification of CEP-5214 and its dimethylglycine ester prodrug clinical candidate CEP-7055. J. Med. Chem. 2003, 46, 5375-5388.
    • (2003) J. Med. Chem. , vol.46 , pp. 5375-5388
    • Gingrich, D.E.1    Reddy, D.R.2    Iqbal, M.A.3    Singh, J.4    Aimone, L.D.5    Angeles, T.S.6    Albom, M.7    Yang, S.8    Ator, M.A.9    Meyer, S.L.10    Robinson, C.11    Ruggeri, B.A.12    Dionne, C.A.13    Vaught, J.L.14    Mallamo, J.P.15    Hudkins, R.L.16
  • 18
  • 19
    • 33645686047 scopus 로고    scopus 로고
    • Quinazoline derivatives as angiogenesis inhibitors. PCT Int. Appl. WO 200047212
    • (b) Hennequin, L.; Stokes, E.; McKerrecher, D. Quinazoline derivatives as angiogenesis inhibitors. PCT Int. Appl. WO 200047212.
    • Hennequin, L.1    Stokes, E.2    McKerrecher, D.3
  • 20
    • 33645669551 scopus 로고    scopus 로고
    • note
    • For the assay conditions of in vitro kinase, cellular proliferation, metabolic stability, cytochrome P450, and pharmacokinetic parameters, see ref 9.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.