Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts. uri icon

abstract

  • Herein we report the synthesis and activity of a novel class of HDAC inhibitors based on 2, 3-diphenyl acrylic acid derivatives. The compounds in this series have shown to be potent HDAC inhibitors possessing significant antiproliferative activity. Further compounds in this series were subjected to metabolic stability in human liver microsomes (HLM), mouse liver microsomes (MLM), and exhibits promising stability in both. These efforts culminated with the identification of a developmental candidate (5a), which displayed desirable PK/PD relationships, significant efficacy in the xenograft models and attractive ADME profiles.

published proceedings

  • Eur J Med Chem

author list (cited authors)

  • Kachhadia, V., Rajagopal, S., Ponpandian, T., Vignesh, R., Anandhan, K., Prabhu, D., ... Gopalan, B.

citation count

  • 5

complete list of authors

  • Kachhadia, Virendra||Rajagopal, Sridharan||Ponpandian, Thanasekaran||Vignesh, Radhakrishnan||Anandhan, Karnambaram||Prabhu, Daivasigamani||Rajendran, Praveen||Nidhyanandan, Saranya||Roy, Anshu Mittal||Ahamed, Fakrudeen Ali||Surendran, Narayanan||Rajagopal, Sriram||Narayanan, Shridhar||Gopalan, Balasubramanian

publication date

  • January 2016