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Quinoline‐Conjugated Ruthenacarboranes: Toward Hybrid Drugs with a Dual Mode of Action

Identifieur interne : 000494 ( Main/Exploration ); précédent : 000493; suivant : 000495

Quinoline‐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-Hawkins

Source :

RBID : PMC:6973020

Abstract

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 closo‐[3‐(η6p‐cymene)‐1‐(quinolin‐8‐yl‐acetate)‐3,1,2‐RuC2B9H10] (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.


Url:
DOI: 10.1002/cmdc.201900349
PubMed: 31675152
PubMed Central: 6973020


Affiliations:


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<name sortKey="Gozzi, Marta" sort="Gozzi, Marta" uniqKey="Gozzi M" first="Marta" last="Gozzi">Marta Gozzi</name>
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