Quinoline‐Conjugated Ruthenacarboranes: Toward Hybrid Drugs with a Dual Mode of Action
Identifieur interne : 000B64 ( Ncbi/Checkpoint ); précédent : 000B63; suivant : 000B65Quinoline‐Conjugated Ruthenacarboranes: Toward Hybrid Drugs with a Dual Mode of Action
Auteurs : Marta Gozzi ; Blagoje Murganic ; Dijana Dra A ; John Popp ; Peter Coburger ; Danijela Maksimovi Vani ; Sanja Mijatovi ; Evamarie Hey-HawkinsSource :
- Chemmedchem [ 1860-7179 ] ; 2019.
Abstract
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
Url:
DOI: 10.1002/cmdc.201900349
PubMed: 31675152
PubMed Central: 6973020
Affiliations:
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<series><title level="j">Chemmedchem</title>
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<front><div type="abstract" xml:lang="en"><title>Abstract</title>
<p>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 <italic>closo</italic>
‐[3‐(<italic>η</italic>
<sup>6</sup>
‐<italic>p</italic>
‐cymene)‐1‐(quinolin‐8‐yl‐acetate)‐3,1,2‐RuC<sub>2</sub>
B<sub>9</sub>
H<sub>10</sub>
] (<bold>4</bold>
) showed a dual mode of action against the LN229 (human glioblastoma) cell line, where it inhibited tumor‐promoting autophagy, and strongly inhibited cell proliferation, <italic>de facto</italic>
blocking cellular division. These results, together with the tendency to spontaneously form nanoparticles in aqueous solution, make complex <bold>4</bold>
a very promising drug candidate for further studies <italic>in vivo</italic>
, for the treatment of autophagy‐prone glioblastomas.</p>
</div>
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<tree><noCountry><name sortKey="Coburger, Peter" sort="Coburger, Peter" uniqKey="Coburger P" first="Peter" last="Coburger">Peter Coburger</name>
<name sortKey="Dra A, Dijana" sort="Dra A, Dijana" uniqKey="Dra A D" first="Dijana" last="Dra A">Dijana Dra A</name>
<name sortKey="Gozzi, Marta" sort="Gozzi, Marta" uniqKey="Gozzi M" first="Marta" last="Gozzi">Marta Gozzi</name>
<name sortKey="Hey Awkins, Evamarie" sort="Hey Awkins, Evamarie" uniqKey="Hey Awkins E" first="Evamarie" last="Hey-Hawkins">Evamarie Hey-Hawkins</name>
<name sortKey="Maksimovi Vani, Danijela" sort="Maksimovi Vani, Danijela" uniqKey="Maksimovi Vani D" first="Danijela" last="Maksimovi Vani">Danijela Maksimovi Vani</name>
<name sortKey="Mijatovi, Sanja" sort="Mijatovi, Sanja" uniqKey="Mijatovi S" first="Sanja" last="Mijatovi">Sanja Mijatovi</name>
<name sortKey="Murganic, Blagoje" sort="Murganic, Blagoje" uniqKey="Murganic B" first="Blagoje" last="Murganic">Blagoje Murganic</name>
<name sortKey="Popp, John" sort="Popp, John" uniqKey="Popp J" first="John" last="Popp">John Popp</name>
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