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Volumn 10, Issue 8, 2000, Pages 767-770

QSAR of 1,1'-(1,2-ethylenebisbenzyl)bis(4-substitutedpyridinium) dibromides as choline kinase inhibitors: A different approach for antiproliferative drug design

Author keywords

[No Author keywords available]

Indexed keywords

CHOLINE KINASE; DIBROMIDE DERIVATIVE; PHOSPHOTRANSFERASE INHIBITOR; UNCLASSIFIED DRUG;

EID: 0342748370     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(00)00080-9     Document Type: Article
Times cited : (34)

References (24)
  • 7
    • 0342924770 scopus 로고    scopus 로고
    • 50 for ChoK inhibition ex vivo is 500 μM using purified ChoK from yeast.
    • 50 for ChoK inhibition ex vivo is 500 μM using purified ChoK from yeast.
  • 9
    • 0343359951 scopus 로고    scopus 로고
    • 50 against the human HT-29 cell line of 2.5 mM.
    • 50 against the human HT-29 cell line of 2.5 mM.
  • 15
    • 0342490583 scopus 로고    scopus 로고
    • Note
    • 50) were calculated using a semilogarithmic plotting of the ratio PCho/(PCho+Cho) versus concentration of the inhibitors.
  • 16
    • 0343359950 scopus 로고    scopus 로고
    • Note
    • Typical procedure: HT-29 cells were grown in Dulbecco's Modified Eagle's medium (DMEM) supplemented with 10% new-born calf serum (NCS) under standard conditions of temperature (37 °C), humidity (95 °C), and carbon dioxide (5%). The cells were seeded on 24-well plates and incubated for 24 h in DMEM supplemented with 10% NCS. Then the cells were washed with TD buffer (137 mM NaCl, 5 mM KCl, 20 mM Tris, pH 7.4) and incubated in DMEM containing the indicated amounts of serum and different concentrations of 5-FU derivatives. Three days later, the wells were aspirated, fresh medium added, and the cells maintained for three additional days. Quantification of the cells remaining in each well was carried out using the Crystal Violet method (See ref 17), with some modifications. Briefly, the cells were washed with TD buffer and fixed with 1% glutaraldehyde for 15 min. After having been washed again with TD, cell nuclei were stained with 0.1% Crystal Violet for at least 30 min, and washed three times with distilled water. Adsorbed dye was resuspended in 10% acetic acid and absorbance at 595 nm was determined in a spectrometer.
  • 20
    • 0343359944 scopus 로고    scopus 로고
    • 3OD at 49.0).
    • 3OD at 49.0).


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.