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Volumn 13, Issue 7, 2003, Pages 1367-1371

Novel and selective imidazole-containing biphenyl inhibitors of protein farnesyltransferase

Author keywords

[No Author keywords available]

Indexed keywords

IMIDAZOLE DERIVATIVE; PROTEIN FARNESYLTRANSFERASE INHIBITOR;

EID: 0037424690     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(03)00096-9     Document Type: Article
Times cited : (19)

References (29)
  • 16
    • 85031209757 scopus 로고    scopus 로고
    • Unpublished data
    • Wang, W. Unpublished data.
    • Wang, W.1
  • 18
    • 0030984431 scopus 로고    scopus 로고
    • For a similar conversion, aniline to methyl benzoate via diazotization/iodination followed by palladium catalyzed carbomethoxylation, see:
    • For a similar conversion, aniline to methyl benzoate via diazotization/iodination followed by palladium catalyzed carbomethoxylation, see: Diaz P., Michel S., Stella L., Charpentier B. Bioorg. Med. Chem. Lett. 7:1997;2289.
    • (1997) Bioorg. Med. Chem. Lett. , vol.7 , pp. 2289
    • Diaz, P.1    Michel, S.2    Stella, L.3    Charpentier, B.4
  • 22
    • 85031201030 scopus 로고    scopus 로고
    • note
    • 1H NMR, mass spectroscopy and elemental analysis.
  • 24
    • 85031197936 scopus 로고    scopus 로고
    • note
    • 50 data were determined against FTase and GGTase1 (purified from bovine brain) using the scintillation proximity assay (SPA). The compounds were assayed once and the reliability of the assay was±50%. See ref 10b for further details.
  • 27
    • 85031198416 scopus 로고    scopus 로고
    • note
    • Subconfluent NIH3T3 ras-transformed cells were used for the Ha-Ras processing assay. The compounds were assayed once and the reliability of the assay was ±50-100%. See ref 10b for further details.
  • 28
    • 85031205153 scopus 로고    scopus 로고
    • note
    • (a) Crystals of rat farnesyltransferase were exposed to compound stabilization solutions for approximately four hours before data collection Diffraction data was collected on a rotating anode source, and a Mar-135 CCD camera system. Data reduction using the HKL2000 program suite yielded a data set which was 98% complete to 2.8 Å, with merging R-values of 4.8% overall. Electron density maps were calculated from models which had been rigid body refined against the data. Models were constructed to fit the observed electron density, and were refined using the XPLOR program package. Final models have R work and R-free values of 24.9 and 32.1% respectively, with no water molecules. Models of this complex have been submitted to the Protein Data Bank (accession 1NL4). (b) Muchmore, S. Unpublished data.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.