title: 5-Aryl-4-(5-substituted-2,4-dihydroxyphenyl)-1,2,3-thiadiazoles as inhibitors of Hsp90 chaperone.
abstract: A series of 5-aryl-4-(5-substituted-2,4-dihydroxyphenyl)-1,2,3-thiadiazoles were synthesized and their binding to several constructs of human Hsp90 chaperone measured by isothermal titration calorimetry (ITC). The most potent compound bound Hsp90 with the dissociation constant of about 5 nM.
authors.affiliation: Laboratory of Biothermodynamics and Drug Design, Insitute of Biotechnology, Graiciuno 8, Vilnius LT-02241, Lithuania.
authors.forename: Inga
authors.initials: I
authors.lastname: Cikotiene
authors.forename: Egidijus
authors.initials: E
authors.lastname: Kazlauskas
authors.forename: Jurgita
authors.initials: J
authors.lastname: Matuliene
authors.forename: Vilma
authors.initials: V
authors.lastname: Michailoviene
authors.forename: Jolanta
authors.initials: J
authors.lastname: Torresan
authors.forename: Jelena
authors.initials: J
authors.lastname: Jachno
authors.forename: Daumantas
authors.initials: D
authors.lastname: Matulis
mesh_terms: D020650:Combinatorial Chemistry Techniques; D004354:Drug Screening Assays, Antitumor; D018841:HSP90 Heat-Shock Proteins / Q000037:antagonists & inhibitors*; D006801:Humans; D018832:Molecular Chaperones / Q000037:antagonists & inhibitors*; D015394:Molecular Structure; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D018841:HSP90 Heat-Shock Proteins; D018832:Molecular Chaperones; D011720:Pyrazoles; D013830:Thiadiazoles