Volume 16, Issue 4 p. 555-558
Communication

Striking Antitumor Activity of a Methinium System with Incorporated Quinoxaline Unit Obtained by Spontaneous Cyclization

T. Bříza

Corresponding Author

T. Bříza

Department of Analytical Chemistry, Institute of Chemical Technology in Prague, Technicka 5, 166 28 Prague 6 (Czech Republic)

First Faculty of Medicine, Charles University in Prague, Kateřinská 32, 121 08 Prague 2 (Czech Republic)

Department of Analytical Chemistry, Institute of Chemical Technology in Prague, Technicka 5, 166 28 Prague 6 (Czech Republic)Search for more papers by this author
J. Králová

J. Králová

Institute of Molecular Genetics, Academy of Sciences of the Czech Republic, Vídeňská 1083, 142 20 Prague 4 (Czech Republic)

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B. Dolenský

B. Dolenský

Department of Analytical Chemistry, Institute of Chemical Technology in Prague, Technicka 5, 166 28 Prague 6 (Czech Republic)

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S. Rimpelová

S. Rimpelová

Department of Biochemistry and Microbiology, Institute of Chemical Technology in Prague, Technicka 5, 166 28 Prague 6 (Czech Republic)

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Z. Kejík

Z. Kejík

Department of Analytical Chemistry, Institute of Chemical Technology in Prague, Technicka 5, 166 28 Prague 6 (Czech Republic)

First Faculty of Medicine, Charles University in Prague, Kateřinská 32, 121 08 Prague 2 (Czech Republic)

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T. Ruml

T. Ruml

Department of Biochemistry and Microbiology, Institute of Chemical Technology in Prague, Technicka 5, 166 28 Prague 6 (Czech Republic)

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M. Hajdúch

M. Hajdúch

Institute of Molecular and Translational Medicine, Hněvotínská 5, 779 00 Olomouc (Czech Republic)

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P. Džubák

P. Džubák

Institute of Molecular and Translational Medicine, Hněvotínská 5, 779 00 Olomouc (Czech Republic)

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I. Mikula

I. Mikula

First Faculty of Medicine, Charles University in Prague, Kateřinská 32, 121 08 Prague 2 (Czech Republic)

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P. Martásek

P. Martásek

First Faculty of Medicine, Charles University in Prague, Kateřinská 32, 121 08 Prague 2 (Czech Republic)

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P. Poučková

P. Poučková

First Faculty of Medicine, Charles University in Prague, Kateřinská 32, 121 08 Prague 2 (Czech Republic)

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V. Král

Corresponding Author

V. Král

Department of Analytical Chemistry, Institute of Chemical Technology in Prague, Technicka 5, 166 28 Prague 6 (Czech Republic)

Department of Analytical Chemistry, Institute of Chemical Technology in Prague, Technicka 5, 166 28 Prague 6 (Czech Republic)Search for more papers by this author
First published: 28 January 2015
Citations: 9

Graphical Abstract

Quinoxaline expansion: The first synthesis of a methinium system with an incorporated quinoxaline unit is presented. This pentamethinium system exerted remarkable biological activity in vivo: it significantly suppressed growth of human breast tumor in nu/nu mice model, thus indicating a promising potential for tumor treatment.

Abstract

A novel pentamethinium salt was synthesized with an unforeseen expanded conjugated quinoxaline unit directly incorporated into a pentamethinium chain. The compound exhibited high fluorescence intensity, selective mitochondrial localization, high cytotoxicity, and selectivity toward malignant cell lines, and resulted in remarkable in vivo suppression of tumor growth in mice.