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KKB Hot Article: Indirubin derivatives as potent FLT3 inhibitors with anti-proliferative activity of acute myeloid leukemic cells |
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Written by KKB
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Tuesday, 20 April 2010 19:55 |
| Citation: Indirubin derivatives as potent FLT3 inhibitors with anti-proliferative activity of acute myeloid leukemic cells |
Authors: Choi SJ, Moon MJ, Lee SD, Choi SU, Han SY, Kim YC.
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| PubMed PMID: 20153646 |
Abstract: Indirubin derivatives were identified as potent FLT3 tyrosine kinase inhibitors with anti-proliferative activity at acute myeloid leukemic cell lines, RS4;11 and MV4;11 which express FLT3-WT and FLT3-ITD mutation, respectively. Among several 5 and 5'-substituted indirubin derivatives, 5-fluoro analog, 13 exhibited potent inhibitory activity at FLT3 (IC(50)=15 nM) with more than 100-fold selectivity versus 6 other kinases and potent anti-proliferative effect for MV4;11 cells (IC(50)=72 nM) with 30-fold selectivity versus RS4;11 cells. Cell cycle analysis indicated that compound 13 induced cell cycle arrest at G(0)/G(1) phase in MV4;11 cells.
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Targets: AURKA,FLT3,KDR
Number of SAR data points: 49
Number of Targets: 3
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Last Updated on Friday, 19 August 2011 23:25 |
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