The Rhodadyns, a new class of small molecule inhibitors of dynamin GTPase activity

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.

Item ID: 36834
Item Type: Article (Research - C1)
ISSN: 1948-5875
Keywords: dynamin inhibition, Knoevengal condensation, rhodanine
Funders: National Medical and Health Research Council (NHMRC), Australian Research Council (ARC), Deutsche Forschungsgemeinschaft (DFG)
Projects and Grants: DFG (SFB765/B4; HA2686/3-2).
Date Deposited: 10 Dec 2014 07:31
FoR Codes: 03 CHEMICAL SCIENCES > 0305 Organic Chemistry > 030503 Organic Chemical Synthesis @ 100%
SEO Codes: 97 EXPANDING KNOWLEDGE > 970103 Expanding Knowledge in the Chemical Sciences @ 100%
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