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Discovery of adamantane based highly potent HDAC inhibitors |
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| Authors: | Balasubramanian Gopalan Thanasekaran Ponpandian Virendra Kachhadia Kuppusamy Bharathimohan Radhakrishnan Vignesh Velaiah Sivasudar Shridhar Narayanan Bhonde Mandar Rajendran Praveen Nithyanandan Saranya Sriram Rajagopal Sridharan Rajagopal |
| Institution: | Drug Discovery Research Centre, Orchid Chemicals & Pharmaceuticals Ltd, Chennai 600119, India |
| 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. |
| Keywords: | Adamantane HDAC inhibitors Nor-adamantane Tumour xenograft |
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