Design,synthesis and anticancer activity of piperazine hydroxamates and their histone deacetylase (HDAC) inhibitory activity |
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| Authors: | Bhadaliya Chetan 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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| Institution: | 1. Department of Pharmaceutical Sciences, Birla Institute of Technology, Mesra, Ranchi, Jharkhand 835 215, India;2. Department of Medical and Chemical Laboratory Diagnostics, General Hospital of Vienna—Medical University of Vienna, Waehringer Guertel 18-20, A-1090 Vienna, Austria;3. Orchid Research Laboratories Ltd, Chennai 600 119, India |
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| 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 GI50 value of 9.33 ± 1.3 μM and 12.03 ± 4 μM, respectively, were tested for their inhibitory potential on hHDAC8. Compound 5c had IC50 of 33.67 μM. 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 IC50 of 0.6 μM at 48 h. |
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