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Bioorg Med Chem Lett. 2009 Feb 15;19(4):1089-92. doi: 10.1016/j.bmcl.2009.01.003. Epub 2009 Jan 9.

5-Aryl-4-(5-substituted-2,4-dihydroxyphenyl)-1,2,3-thiadiazoles as inhibitors of Hsp90 chaperone.

Author information

1
Laboratory of Biothermodynamics and Drug Design, Insitute of Biotechnology, Graiciuno 8, Vilnius LT-02241, Lithuania.

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.

PMID:
19168355
DOI:
10.1016/j.bmcl.2009.01.003
[Indexed for MEDLINE]

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