Design, synthesis and anticancer activity of piperazine hydroxamates and their histone deacetylase (HDAC) inhibitory activity. Academic Article uri icon


  • 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.

published proceedings

  • Bioorg Med Chem Lett

author list (cited authors)

  • Chetan, B., Bunha, M., Jagrat, M., Sinha, B. N., Saiko, P., Graser, G., ... Jayaprakash, V.

complete list of authors

  • Chetan, Bhadaliya||Bunha, Mahesh||Jagrat, Monika||Sinha, Barij Nayan||Saiko, Philipp||Graser, Geraldine||Szekeres, Thomas||Raman, Ganapathy||Rajendran, Praveen||Moorthy, Dhatchana||Basu, Arijit||Jayaprakash, Venkatesan

publication date

  • July 2010