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Volumn 21, Issue 18, 2011, Pages 5239-5243

Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1α inhibitors

Author keywords

Hypoxia inducible factor 1 ; Parallel synthesis; Quinazolin 4 ones

Indexed keywords

HYPOXIA INDUCIBLE FACTOR 1ALPHA; PROTEIN INHIBITOR; QUINAZOLIN 4 ONE ANALOG; QUINAZOLINONE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 80051923846     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.07.043     Document Type: Article
Times cited : (9)

References (29)
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    • 80051951509 scopus 로고    scopus 로고
    • Note
    • + 365.1983, found 365.1982.
  • 24
    • 80051945924 scopus 로고    scopus 로고
    • Note
    • TM B/G FRET substrate (Invitrogen, Carlsbad, CA) mixture was added into the plates, the assay plates were incubated at room temperature for 2.5 h, and the fluorescence intensity (405 nm excitation, and 460 and 530 nm emissions) was measured by an Envision plate reader (Perkin Elmer, Shelton CT).
  • 25
    • 80051944740 scopus 로고    scopus 로고
    • Note
    • 6 HRE-bla ME-180 cells per well were cultured in a 6-well plate. After 6 h, the cells were treated for 17 h with DMSO in a normal atmosphere (negative control) and 1% oxygen (positive control), or with 1 or 10 μM solutions of 16 or 18 in DMSO at 1% oxygen. After the treatment, the cells were lysed in lysis buffer (Invitrogen) containing 1% of protease inhibitor (Sigma) for 10 min on ice. After the samples were centrifuged for 10 min at 14000 rpm and 4 °C, supernatants were collected and subjected to SDS-PAGE analysis on a 10% Tris-Glycine gel (Invitrogen). Same amount of protein (25 μg) from each sample was loaded into the gel. Proteins were transferred to a PVDF membrane (Invitrogen) and the membrane was blotted with primary antibodies against HIF-1α at a 1:250 dilution (Santa Cruz Biotechnologies, Santa Cruz, CA) or β-Actin at 1:5000 dilution (Sigma) as a loading control. HRP conjugated secondary antibody (1:1000 dilution; anti-goat anti-rabbit or anti-mouse, Santa Cruz, CA) was used together with the Western Blot Luminol reagent kit (Santa Cruz Biotechnology, CA) to develop the membrane that was read with the ChemiDoc XRS system (Bio-Rad, Hercules, CA).


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.