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Volumn 20, Issue 23, 2010, Pages 6895-6898

Identification and structure-activity relationship of 2-morpholino 6-(3-hydroxyphenyl) pyrimidines, a class of potent and selective PI3 kinase inhibitors

Author keywords

2 Morpholino pyrimidines; Cancer treatment; Phosphoinositol; PI3 Kinase; PI3 Kinase inhibitors

Indexed keywords

2 MORPHOLINO 6 (3 HYDROXYPHENYL)PYRIMIDINE; PHOSPHATIDYLINOSITOL 3 KINASE; PHOSPHATIDYLINOSITOL 3 KINASE INHIBITOR; PROTEIN KINASE B; PYRIMIDINE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 78149283201     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.10.021     Document Type: Article
Times cited : (26)

References (20)
  • 16
    • 78149282853 scopus 로고    scopus 로고
    • note
    • 2O, 300 MHz): δ ppm 8.09 (s, 1H), 8.03 (br s, 1H), 7.61 (d, 1H, J = 7.8 Hz), 7.55 (br m, 1H), 7.38 (app. t, 1H, J = 7.8 Hz), 7.17 (br d, 1H, J = 7.8 Hz), 7.10 (br s, 1H), 7.06 (d, 1H, J = 8.7 Hz), 6.42 (br s, 1H), 3.75 (br s, 8H); LCMS m/z (%): 389.2 (M+H).
  • 17
    • 78149283887 scopus 로고    scopus 로고
    • note
    • The model for compound in p110α was built in Maestro 8.0.308 after merging the compound 25 coordinates from a Novartis structure of the compound bound to PI3K p110γ (PDB accession code: 3P2B) with the aligned coordinates of the public domain p110α apo-structure (PDB deposition code: 2RD0). All key protein-compound interactions are retained between the p110γ structure and the p110α model and no new interactions are expected with the other PI3K Class I isoforms.
  • 18
    • 78149284229 scopus 로고    scopus 로고
    • 50 is 0.55 μM for 25
    • 50 is 0.55 μM for 25.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.