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

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

Affiliation

  • 1 Zydus Research Centre, Medicinal Chemistry, Sarkhej-Bavla N. H.8A, Moraiya, Ahmedabad, Gujarat 382210, India. saurinraval@zyduscadila.com
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.

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