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Volumn 19, Issue 3, 2009, Pages 644-649

SAR and biological evaluation of analogues of a small molecule histone deacetylase inhibitor N-(2-aminophenyl)-4-((4-(pyridin-3-yl)pyrimidin-2-ylamino)methyl)benzamide (MGCD0103)

Author keywords

Class I; HDAC; Inhibitors; MGCD0103; Oncology

Indexed keywords

CYCLIN DEPENDENT KINASE INHIBITOR 1; HISTONE DEACETYLASE 1; HISTONE DEACETYLASE INHIBITOR; N (2 AMINOPHENYL) 4 [4 (3 PYRIDINYL) 2 PYRIMIDINYLAMINOMETHYL]BENZAMIDE;

EID: 58549105898     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.12.048     Document Type: Article
Times cited : (8)

References (16)
  • 1
    • 34547897023 scopus 로고    scopus 로고
    • For a review see
    • For a review see. Glozak M., and Seto E. Oncogene 26 (2007) 5420
    • (2007) Oncogene , vol.26 , pp. 5420
    • Glozak, M.1    Seto, E.2
  • 11
    • 58549096740 scopus 로고    scopus 로고
    • note
    • The details for the synthesis and the characterization of all the new compounds are described in PCT WO 2003/024448 A2, WO 2004/035525 A1, and WO 2005/092899 A1. All compounds were initially screened for their ability to inhibit recombinant human HDAC1. We targeted this isotype following the results of our work and of others which implicated HDAC1 for both transcriptional repression and chromatin remodeling (Carmen, A. A.; Rundlett, S. E.; Grunstein, M. J. Biol. Chem. 1996, 271, 15837). The compounds were screened as described earlier, using Boc_Lys(acetyl)-AMC as substrate. The in vitro anti-proliferative activities of the synthesized compounds against HCT116 human colon cancer cell line were evaluated using 3-[4,5-dimethylthiazol-2-yl-2,5-diphenyltetrazolium bromide (MTT).
  • 14
    • 58549106799 scopus 로고    scopus 로고
    • US Patent 6174905, 2001.
    • US Patent 6174905, 2001.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.