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Volumn 17, Issue 21, 2007, Pages 5995-5999

Design and synthesis of thiazole-5-hydroxamic acids as novel histone deacetylase inhibitors

Author keywords

Antiproliferative; HDAC; Inhibitors; Synthesis

Indexed keywords

4 METHYLPHENYLSULFONAMIDE DERIVATIVE; CHELATING AGENT; HISTONE DEACETYLASE INHIBITOR; HYDROXAMIC ACID DERIVATIVE; PIPERAZINE DERIVATIVE; SULFONAMIDE; THIAZOLE 5 HYDROXAMIC ACID DERIVATIVE; THIAZOLE DERIVATIVE; UNCLASSIFIED DRUG; ZINC DERIVATIVE;

EID: 34548853387     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.07.050     Document Type: Article
Times cited : (29)

References (26)
  • 25
    • 34548853857 scopus 로고    scopus 로고
    • note
    • In vitro fluorescent histone deacetylase assay: HDAC inhibition assays were performed using the HDAC fluorescent activity assay kit (Biomol Research Laboratories, Plymouth Meeting, PA). HeLa cell nuclear extract, which contains a number of HDAC isozymes and other nuclear factors, was used as the source of HDAC activity. The final substrate concentration in the assay mixture was 50 μM. The reaction was allowed to proceed for 10 min at room temperature before a stop solution was added. Test compounds were prepared as 20 mM stock solutions in DMSO (Molecular Biology grade, Sigma-Aldrich Co., St. Louis, MO) and stored at -70 °C. DMSO had no significant effect on the activity of this assay at concentrations up to 5% with the final DMSO concentration in the assays of no more than 2%. Assays were performed in white polystyrene 96-well half-area assay plates (Corning, Corning, NY) and measured on a Wallac 1420 fluorescent plate reader (Wallac Oy, Turku, Finland) with an excitation wavelength of 355 nm, an emission wavelength of 460 nm, and a one sec signal averaging time.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.