title: Design and synthesis of novel 3-hydroxy-cyclobut-3-ene-1,2-dione derivatives as thyroid hormone receptor beta (TR-beta) selective ligands.
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.
authors.affiliation: Zydus Research Centre, Medicinal Chemistry, Sarkhej-Bavla N. H.8A, Moraiya, Ahmedabad, Gujarat 382210, India. saurinraval@zyduscadila.com
authors.forename: Saurin
authors.initials: S
authors.lastname: Raval
authors.forename: Preeti
authors.initials: P
authors.lastname: Raval
authors.forename: Debdutta
authors.initials: D
authors.lastname: Bandyopadhyay
authors.forename: Krunal
authors.initials: K
authors.lastname: Soni
authors.forename: Digambar
authors.initials: D
authors.lastname: Yevale
authors.forename: Digvijay
authors.initials: D
authors.lastname: Jogiya
authors.forename: Honey
authors.initials: H
authors.lastname: Modi
authors.forename: Amit
authors.initials: A
authors.lastname: Joharapurkar
authors.forename: Neha
authors.initials: N
authors.lastname: Gandhi
authors.forename: Mukul R
authors.initials: MR
authors.lastname: Jain
authors.forename: Pankaj R
authors.initials: PR
authors.lastname: Patel
mesh_terms: D002626:Chemistry, Pharmaceutical / Q000379:methods; D018360:Crystallography, X-Ray; D003503:Cyclobutanes / Q000737:chemistry*; D015195:Drug Design; D006801:Humans; D008024:Ligands; D008156:Luciferases / Q000378:metabolism; D008956:Models, Chemical; D008968:Molecular Conformation; D010647:Phenyl Ethers / Q000494:pharmacology; D010648:Phenylacetates / Q000494:pharmacology; D011485:Protein Binding; D013329:Structure-Activity Relationship; D013961:Thyroid Gland / Q000201:enzymology; D037021:Thyroid Hormone Receptors alpha / Q000378:metabolism; D037042:Thyroid Hormone Receptors beta / Q000737:chemistry* / Q000378:metabolism*
chemical_list: C110624:3-cyclobutene-1,2-dione; D003503:Cyclobutanes; C478108:KB 141; D008024:Ligands; D010647:Phenyl Ethers; D010648:Phenylacetates; D037021:Thyroid Hormone Receptors alpha; D037042:Thyroid Hormone Receptors beta; D008156:Luciferases