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Quinoline‐Conjugated Ruthenacarboranes: Toward Hybrid Drugs with a Dual Mode of Action
The role of autophagy in cancer is often complex, ranging from tumor‐promoting to ‐suppressing effects. In this study, two novel hybrid molecules were designed, containing a ruthenacarborane fragment conjugated with a known modulator of autophagy, namely a quinoline derivative. The complex closo‐[3‐...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
John Wiley and Sons Inc.
2019
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6973020/ https://www.ncbi.nlm.nih.gov/pubmed/31675152 http://dx.doi.org/10.1002/cmdc.201900349 |
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author | Gozzi, Marta Murganic, Blagoje Drača, Dijana Popp, John Coburger, Peter Maksimović‐Ivanić, Danijela Mijatović, Sanja Hey‐Hawkins, Evamarie |
author_facet | Gozzi, Marta Murganic, Blagoje Drača, Dijana Popp, John Coburger, Peter Maksimović‐Ivanić, Danijela Mijatović, Sanja Hey‐Hawkins, Evamarie |
author_sort | Gozzi, Marta |
collection | PubMed |
description | The role of autophagy in cancer is often complex, ranging from tumor‐promoting to ‐suppressing effects. In this study, two novel hybrid molecules were designed, containing a ruthenacarborane fragment conjugated with a known modulator of autophagy, namely a quinoline derivative. The complex closo‐[3‐(η (6)‐p‐cymene)‐1‐(quinolin‐8‐yl‐acetate)‐3,1,2‐RuC(2)B(9)H(10)] (4) showed a dual mode of action against the LN229 (human glioblastoma) cell line, where it inhibited tumor‐promoting autophagy, and strongly inhibited cell proliferation, de facto blocking cellular division. These results, together with the tendency to spontaneously form nanoparticles in aqueous solution, make complex 4 a very promising drug candidate for further studies in vivo, for the treatment of autophagy‐prone glioblastomas. |
format | Online Article Text |
id | pubmed-6973020 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | John Wiley and Sons Inc. |
record_format | MEDLINE/PubMed |
spelling | pubmed-69730202020-01-27 Quinoline‐Conjugated Ruthenacarboranes: Toward Hybrid Drugs with a Dual Mode of Action Gozzi, Marta Murganic, Blagoje Drača, Dijana Popp, John Coburger, Peter Maksimović‐Ivanić, Danijela Mijatović, Sanja Hey‐Hawkins, Evamarie ChemMedChem Full Papers The role of autophagy in cancer is often complex, ranging from tumor‐promoting to ‐suppressing effects. In this study, two novel hybrid molecules were designed, containing a ruthenacarborane fragment conjugated with a known modulator of autophagy, namely a quinoline derivative. The complex closo‐[3‐(η (6)‐p‐cymene)‐1‐(quinolin‐8‐yl‐acetate)‐3,1,2‐RuC(2)B(9)H(10)] (4) showed a dual mode of action against the LN229 (human glioblastoma) cell line, where it inhibited tumor‐promoting autophagy, and strongly inhibited cell proliferation, de facto blocking cellular division. These results, together with the tendency to spontaneously form nanoparticles in aqueous solution, make complex 4 a very promising drug candidate for further studies in vivo, for the treatment of autophagy‐prone glioblastomas. John Wiley and Sons Inc. 2019-11-19 2019-12-17 /pmc/articles/PMC6973020/ /pubmed/31675152 http://dx.doi.org/10.1002/cmdc.201900349 Text en ©2019 The Authors. Published by Wiley-VCH Verlag GmbH & Co. KGaA. This is an open access article under the terms of the http://creativecommons.org/licenses/by/4.0/ License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Full Papers Gozzi, Marta Murganic, Blagoje Drača, Dijana Popp, John Coburger, Peter Maksimović‐Ivanić, Danijela Mijatović, Sanja Hey‐Hawkins, Evamarie Quinoline‐Conjugated Ruthenacarboranes: Toward Hybrid Drugs with a Dual Mode of Action |
title | Quinoline‐Conjugated Ruthenacarboranes: Toward Hybrid Drugs with a Dual Mode of Action |
title_full | Quinoline‐Conjugated Ruthenacarboranes: Toward Hybrid Drugs with a Dual Mode of Action |
title_fullStr | Quinoline‐Conjugated Ruthenacarboranes: Toward Hybrid Drugs with a Dual Mode of Action |
title_full_unstemmed | Quinoline‐Conjugated Ruthenacarboranes: Toward Hybrid Drugs with a Dual Mode of Action |
title_short | Quinoline‐Conjugated Ruthenacarboranes: Toward Hybrid Drugs with a Dual Mode of Action |
title_sort | quinoline‐conjugated ruthenacarboranes: toward hybrid drugs with a dual mode of action |
topic | Full Papers |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6973020/ https://www.ncbi.nlm.nih.gov/pubmed/31675152 http://dx.doi.org/10.1002/cmdc.201900349 |
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