Discovery of adamantane based highly potent HDAC inhibitors. Academic Article

abstract

• Herein, we report the development of highly potent HDAC inhibitors for the treatment of cancer. A series of adamantane and nor-adamantane based HDAC inhibitors were designed, synthesized and screened for the inhibitory activity of HDAC. A number of compounds exhibited GI50 of 10-100 nM in human HCT116, NCI-H460 and U251 cancer cells, in vitro. Compound 32 displays efficacy in human tumour animal xenograft model.

authors

• Rajendran, Praveen

published proceedings

• Bioorg Med Chem Lett

altmetric score

• 6.25

author list (cited authors)

• Gopalan, B., Ponpandian, T., Kachhadia, V., Bharathimohan, K., Vignesh, R., Sivasudar, V., ... Rajagopal, S.

citation count

• 33

complete list of authors

• Gopalan, Balasubramanian||Ponpandian, Thanasekaran||Kachhadia, Virendra||Bharathimohan, Kuppusamy||Vignesh, Radhakrishnan||Sivasudar, Velaiah||Narayanan, Shridhar||Mandar, Bhonde||Praveen, Rajendran||Saranya, Nithyanandan||Rajagopal, Sriram||Rajagopal, Sridharan

publication date

• May 2013

publisher

• Elsevier  Publisher

published in

• Bioorganic and Medicinal Chemistry Letters  Journal

keywords

• Adamantane
• Animals
• Antineoplastic Agents
• Cell Line, Tumor
• Cell Survival
• Drug Evaluation, Preclinical
• Drug Screening Assays, Antitumor
• HCT116 Cells
• Histone Deacetylase Inhibitors
• Histone Deacetylases
• Humans
• Lung Neoplasms
• Mice
• Mice, SCID
• Structure-Activity Relationship
• Transplantation, Heterologous

Digital Object Identifier (DOI)

• 10.1016/j.bmcl.2013.03.002

start page

• 2532

end page

• 2537

volume

• 23

issue

• 9

URL

• http://dx.doi.org/10.1016/j.bmcl.2013.03.002