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Addition of 2-(ethylamino)acetonitrile group to nitroxoline results in significantly improved anti-tumor activity in vitro and in vivo [Elektronski vir]Mitrović, Ana ...Lysosomal cysteine peptidase cathepsin B, involved in multiple processes associated with tumor progression, is validated as a target for anti-cancer therapy. Nitroxoline, a known antimicrobial agent, ... is a potent and selective inhibitor of cathepsin B, hence reducing tumor progression in vitro and in vivo. In order to further improve its anti-cancer properties we developed a number of derivatives using structure-based chemical synthesis. Of these, the 7-aminomethylated derivative (compound 17) exhibited significantly improved kinetic properties over nitroxoline, inhibiting cathepsin B endopeptidase activity selectively. In the present study, we have evaluated its anti-cancer properties. It was more effective than nitroxoline in reducing tumor cell invasion and migration, as determined in vitro on two-dimensional cell models and tumor spheroids, under either endpoint or real time conditions. Moreover, it exhibited improved action over nitroxoline in impairing tumor growth in vivo in LPB mouse fibrosarcoma tumors in C57Bl/6 mice. Taken together, the addition of a 2-(ethylamino)acetonitrile group to nitroxoline at position 7 significantly improves its pharmacological characteristics and its potential for use as an anti-cancer drug.Source: Oncotarget [Elektronski vir]. - ISSN 1949-2553 (Vol. 8, no. 35, 2017, str. 59136-59147)Type of material - e-article ; adult, seriousPublish date - 2017Language - englishCOBISS.SI-ID - 4360305
Author
Mitrović, Ana |
Sosič, Izidor |
Kos, Špela, farmacija |
Lampreht Tratar, Urša |
Breznik, Barbara, 1989- |
Kranjc Brezar, Simona |
Mirković, Bojana |
Gobec, Stanislav, 1970- |
Lah Turnšek, Tamara |
Čemažar, Maja |
Serša, Gregor |
Kos, Janko, 1959-
Topics
nitroxoline derivative |
cathepsin B |
inhibition |
tumor invasion |
cell migration
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Author | Mitrović, Ana ... |
Title | Addition of 2-(ethylamino)acetonitrile group to nitroxoline results in significantly improved anti-tumor activity in vitro and in vivo [Elektronski vir] |
Publication date | 2017-07-17 |
COBISS.SI-ID | 4360305 |
Publication version in repository | Publisher's version |
Publication licence | Creative Commons Attribution 4.0 International |
Embargo | Immediate publication for public |
Project(s) from which the publication was funded
Title | Acronym | Project ID | Funder |
---|---|---|---|
Nitroksolin in njegovi derivati kot nova protitumorska zdravila | J4-5529-2013 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
|
Farmacevtska biotehnologija: znanost za zdravje | P4-0127-2015 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
|
Strukturno podprta optimizacija na nitroksolinu osnovanih zaviralcev katepsina B kot potencialnih zdravil za zdravljenje raka | Z1-7181-2016 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
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Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Mitrović, Ana | 36440 |
Sosič, Izidor | 30816 |
Kos, Špela, farmacija | 36366 |
Lampreht Tratar, Urša | 36367 |
Breznik, Barbara, 1989- | 36319 |
Kranjc Brezar, Simona | 19058 |
Mirković, Bojana | 29604 |
Gobec, Stanislav, 1970- | 15284 |
Lah Turnšek, Tamara | 07802 |
Čemažar, Maja | 14575 |
Serša, Gregor | 08800 |
Kos, Janko, 1959- | 04648 |
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