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ACS Med Chem Lett. 2012 Mar 26;3(5):352-6. doi: 10.1021/ml200284s. eCollection 2012 May 10.

The Rhodadyns, a New Class of Small Molecule Inhibitors of Dynamin GTPase Activity.

Author information

1
Chemistry, The University of Newcastle , University Drive, Callaghan, NSW 2308, Australia.
2
Cell Signalling Unit, Children's Medical Research Institute, The University of Sydney , Sydney, NSW 2145, Australia.
3
Leibniz Institut für Molekulare Pharmakologie & Freie Universität Berlin , 13125 Berlin, Germany.

Abstract

Six focused rhodanine-based libraries, 60 compounds in total, were synthesized and evaluated as potential dynamin I GTPase inhibitors. Twenty-six were more potent than the lead compound with 13 returning IC50 values ≤10 μM, making the Rhodadyn series among the most active dynamin inhibitors reported. Two analogues were highly effective at blocking receptor-mediated endocytosis: C10 and D10 with IC50(RME) = 7.0 ± 2.2 and 5.9 ± 1.0 μM, respectively. These compounds are equipotent with the best reported in-cell dynamin inhibitors.

KEYWORDS:

Knoevengal condensation; dynamin inhibition; rhodanine

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