Design, synthesis and anticancer activity of piperazine hydroxamates and their histone deacetylase (HDAC) inhibitory activity

Bioorg Med Chem Lett. 2010 Jul 1;20(13):3906-10. doi: 10.1016/j.bmcl.2010.05.020.

Bhadaliya Chetan ¹, Mahesh Bunha, Monika Jagrat, Barij Nayan Sinha, Philipp Saiko, Geraldine Graser, Thomas Szekeres, Ganapathy Raman, Praveen Rajendran, Dhatchana Moorthy, Arijit Basu, Venkatesan Jayaprakash

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1 Department of Pharmaceutical Sciences, Birla Institute of Technology, Mesra, Ranchi, Jharkhand, India.

PMID: 20605448 DOI: 10.1016/j.bmcl.2010.05.020

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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