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

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.

authors

• Rajendran, Praveen

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.

citation count

• 41

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

publisher

• Elsevier  Publisher

published in

• Bioorganic and Medicinal Chemistry Letters  Journal

keywords

• Antineoplastic Agents
• Cell Line, Tumor
• Cell Proliferation
• Cell Survival
• Dose-Response Relationship, Drug
• Drug Design
• Drug Screening Assays, Antitumor
• Histone Deacetylase Inhibitors
• Histone Deacetylases
• Humans
• Hydroxamic Acids
• Models, Molecular
• Molecular Structure
• Piperazine
• Piperazines
• Stereoisomerism
• Structure-Activity Relationship

PubMed Central ID

• 20605448

Digital Object Identifier (DOI)

• 10.1016/j.bmcl.2010.05.020

start page

• 3906

end page

• 3910

volume

• 20

issue

• 13

URL

• http://dx.doi.org/10.1016/j.bmcl.2010.05.020