Design and synthesis of novel 3-hydroxy-cyclobut-3-ene-1,2-dione derivatives as thyroid hormone receptor beta (TR-beta) selective ligands

  • Bioorg Med Chem Lett. 2008 Jul 15;18(14):3919-24. doi: 10.1016/j.bmcl.2008.06.038.
Saurin Raval  1 ,  Preeti Raval ,  Debdutta Bandyopadhyay ,  Krunal Soni ,  Digambar Yevale ,  Digvijay Jogiya ,  Honey Modi ,  Amit Joharapurkar ,  Neha Gandhi ,  Mukul R Jain ,  Pankaj R Patel
Affiliations
  • 1. Zydus Research Centre, Medicinal Chemistry, Sarkhej-Bavla N. H.8A, Moraiya, Ahmedabad, Gujarat 382210, India. [email protected]
PMID: 18585912 DOI: 10.1016/j.bmcl.2008.06.038
Abstract

Design and synthesis of a novel 3-hydroxy-cyclobut-3-ene-1,2-dione derivatives are reported and their in vitro Thyroid Hormone Receptor selectivity has been evaluated in the thyroid luciferase receptor assay. The 3-[3,5-dichloro-4-(4-hydroxy-3-isopropylphenoxy)-phenylamino]-4-hydroxy-cyclobut-3-ene-1,2-dione 21 has shown selectivity towards Thyroid Hormone Receptor beta.