Discovery of adamantane based highly potent HDAC inhibitors
B Gopalan, T Ponpandian, V Kachhadia… - Bioorganic & medicinal …, 2013 - Elsevier
B Gopalan, T Ponpandian, V Kachhadia, K Bharathimohan, R Vignesh, V Sivasudar…
Bioorganic & medicinal chemistry letters, 2013•ElsevierHerein, 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.
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.
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.
Elsevier
