Literature DB >> 19168355

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

Inga Cikotiene1, Egidijus Kazlauskas, Jurgita Matuliene, Vilma Michailoviene, Jolanta Torresan, Jelena Jachno, Daumantas Matulis.   

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.

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Year:  2009        PMID: 19168355     DOI: 10.1016/j.bmcl.2009.01.003

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  8 in total

1.  Volume of Hsp90 ligand binding and the unfolding phase diagram as a function of pressure and temperature.

Authors:  Vytautas Petrauskas; Joana Gylytė; Zigmantas Toleikis; Piotras Cimmperman; Daumantas Matulis
Journal:  Eur Biophys J       Date:  2013-01-05       Impact factor: 1.733

2.  Synthesis of 2-(2,4-dihydroxyphenyl)thieno-1,3-thiazin-4-ones, their lipophilicity and anticancer activity in vitro.

Authors:  Joanna Matysiak; Małgorzata Juszczak; Monika M Karpińska; Ewa Langner; Katarzyna Walczak; Marta K Lemieszek; Alicja Skrzypek; Andrzej Niewiadomy; Wojciech Rzeski
Journal:  Mol Divers       Date:  2015-04-29       Impact factor: 2.943

3.  Thermodynamics of aryl-dihydroxyphenyl-thiadiazole binding to human Hsp90.

Authors:  Egidijus Kazlauskas; Vilma Petrikaitė; Vilma Michailovienė; Jurgita Revuckienė; Jurgita Matulienė; Leonas Grinius; Daumantas Matulis
Journal:  PLoS One       Date:  2012-05-24       Impact factor: 3.240

4.  Synthesis, characterization, and pharmacological evaluation of novel azolo- and azinothiazinones containing 2,4-dihydroxyphenyl substituent as anticancer agents.

Authors:  Joanna Matysiak; Małgorzata Juszczak; Monika M Karpińska; Ewa Langner; Katarzyna Walczak; Marta Lemieszek; Alicja Skrzypek; Wojciech Rzeski; Andrzej Niewiadomy
Journal:  Monatsh Chem       Date:  2015-04-02       Impact factor: 1.451

5.  I2/DMSO-Catalyzed Transformation of N-tosylhydrazones to 1,2,3-thiadiazoles.

Authors:  Weiwei Li; Jun Zhang; Jing He; Liang Xu; Luigi Vaccaro; Ping Liu; Yanlong Gu
Journal:  Front Chem       Date:  2020-06-12       Impact factor: 5.221

6.  Synergistic activity of Hsp90 inhibitors and anticancer agents in pancreatic cancer cell cultures.

Authors:  Simonas Daunys; Daumantas Matulis; Vilma Petrikaitė
Journal:  Sci Rep       Date:  2019-11-07       Impact factor: 4.379

Review 7.  Thiadiazole derivatives as anticancer agents.

Authors:  Monika Szeliga
Journal:  Pharmacol Rep       Date:  2020-09-03       Impact factor: 3.024

8.  Co-crystalization and in vitro biological characterization of 5-aryl-4-(5-substituted-2-4-dihydroxyphenyl)-1,2,3-thiadiazole Hsp90 inhibitors.

Authors:  Swee Y Sharp; S Mark Roe; Egidijus Kazlauskas; Inga Cikotienė; Paul Workman; Daumantas Matulis; Chrisostomos Prodromou
Journal:  PLoS One       Date:  2012-09-11       Impact factor: 3.240

  8 in total

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