Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 13, Pages 3906-3910Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.05.020
Keywords
Histone deacetylase inhibitors; Piperazine linker; Hydroxamates; RR pharmacophore
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Funding
- UGC
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Six compounds were synthesized with piperazine in linker region and hydroxamate as Zinc Binding Group ( ZBG). They were screened against three cancer cell-lines (NCIH460; HCT116; U251). Compounds 5c and 5f with GI(50) value of 9.33 +/- 1.3 mu M and 12.03 +/- 4 mu M, respectively, were tested for their inhibitory potential on hHDAC8. Compound 5c had IC(50) of 33.67 mu M. Compounds were also screened for their anticancer activity against HL60 human promyelocytic leukemia cell line due to the presence of pharmacophoric features of RR inhibitors in them. Compound 5c had IC(50) of 0.6 mu M at 48 h. (c) 2010 Elsevier Ltd. All rights reserved.
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