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  • Title: Design, synthesis and anticancer activity of piperazine hydroxamates and their histone deacetylase (HDAC) inhibitory activity.
    Author: Chetan B, Bunha M, Jagrat M, Sinha BN, Saiko P, Graser G, Szekeres T, Raman G, Rajendran P, Moorthy D, Basu A, Jayaprakash V.
    Journal: Bioorg Med Chem Lett; 2010 Jul 01; 20(13):3906-10. PubMed ID: 20605448.
    Abstract:
    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 microM and 12.03+/-4 microM, respectively, were tested for their inhibitory potential on hHDAC8. Compound 5c had IC(50) of 33.67 microM. 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 microM at 48h.
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