Robertson, Mark J., Hadzic, Gordana, Ambrus, Joseph, Pomè, D. Yuri, Hyde, Emily, Whiting, Ainslie, Mariana, Anna, von Keist, Lisa, Chau, Ngoc, Haucke, Volker, Robinson, Phillip J., and McCluskey, Adam (2012) The Rhodadyns, a new class of small molecule inhibitors of dynamin GTPase activity. ACS Medicinal Chemistry Letters, 3 (5). pp. 352-356.

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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.

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