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  3. Discovery of adamantane based highly potent HDAC inhibitors

Discovery of adamantane based highly potent HDAC inhibitors

  • Bioorg Med Chem Lett. 2013 May 1;23(9):2532-7. doi: 10.1016/j.bmcl.2013.03.002.
Balasubramanian Gopalan 1,  Thanasekaran Ponpandian,  Virendra Kachhadia,  Kuppusamy Bharathimohan,  Radhakrishnan Vignesh,  Velaiah Sivasudar,  Shridhar Narayanan,  Bhonde Mandar,  Rajendran Praveen,  Nithyanandan Saranya,  Sriram Rajagopal,  Sridharan Rajagopal
Affiliations

Affiliation

  • 1 Drug Discovery Research Centre, Orchid Chemicals & Pharmaceuticals Ltd, Chennai 600119, India.
PMID: 23538115 DOI: 10.1016/j.bmcl.2013.03.002
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.

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