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Volumn 19, Issue 20, 2009, Pages 5950-5953

The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase

Author keywords

Antitumour; mTOR; Serine threonine kinase

Indexed keywords

KU 63794; MAMMALIAN TARGET OF RAPAMYCIN; MAMMALIAN TARGET OF RAPAMYCIN C1; MAMMALIAN TARGET OF RAPAMYCIN C2; MAMMALIAN TARGET OF RAPAMYCIN INHIBITOR; PHOSPHATIDYLINOSITOL 3 KINASE; PYRIDO[2,3 D]PYRIMIDINE 2,4 DIAMINE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 70349256453     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.08.038     Document Type: Article
Times cited : (82)

References (22)
  • 13
    • 70349255180 scopus 로고    scopus 로고
    • note
    • Inhibition of mTOR kinase was assayed using full-length mTOR (extracted from HeLa cytoplasmic extract by immunoprecipitation) with a recombinant 4E-BP1 protein substrate and an ATP concentration of 50 μM. Detection of phosphorylated product through an ELISA format was essentially as described in Ref. 8. Figures quoted are the mean of at least 3 determinations and variability around the mean was <50%.
  • 14
    • 70349250801 scopus 로고    scopus 로고
    • note
    • Compounds (2), (3) and (4) were prepared according to the same methods described in Scheme 1 from 3-amino-isonicotinic acid, 3-aminopicolinic acid and anthranilic acid, respectively.
  • 15
    • 70349245948 scopus 로고    scopus 로고
    • BioByte Version 4.3
    • BioByte www.biobyte.com CLog P Version 4.3.
  • 19
    • 70349233391 scopus 로고    scopus 로고
    • note
    • Typical Buchwald conditions: (18), relevant amine, tris(dibenzylideneacetone)dipalladium(0), Xantphos, cesium carbonate, dioxane, 150 °C, 40 min.
  • 20
    • 70349253564 scopus 로고    scopus 로고
    • note
    • 2O, 95 °C, 2 h.
  • 21
    • 70349233390 scopus 로고    scopus 로고
    • Hummersone, M. G.; Gomez, S.; Menear, K. A.; Smith, G. C. M.; Malagu, K.; Duggan, H. M. E.; Cockcroft, X.-L. F.; Hermann, G. J. WO2007060404, 2007.
    • Hummersone, M. G.; Gomez, S.; Menear, K. A.; Smith, G. C. M.; Malagu, K.; Duggan, H. M. E.; Cockcroft, X.-L. F.; Hermann, G. J. WO2007060404, 2007.
  • 22
    • 70349248935 scopus 로고    scopus 로고
    • Bailey, J. P.; Giles, M. B.; Pass, M. WO2006005914, 2006.
    • Bailey, J. P.; Giles, M. B.; Pass, M. WO2006005914, 2006.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.