The Rhodadyns, a New Class of Small Molecule Inhibitors of Dynamin GTPase Activity.
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ABSTRACT:
SUBMITTER: Robertson MJ
PROVIDER: S-EPMC4025782 | biostudies-other | 2012 May
REPOSITORIES: biostudies-other
Publications
The Rhodadyns, a New Class of Small Molecule Inhibitors of Dynamin GTPase Activity.
Robertson Mark J MJ Hadzic Gordana G Ambrus Joseph J Pomè D Yuri DY Hyde Emily E Whiting Ainslie A Mariana Anna A von Kleist Lisa L Chau Ngoc N Haucke Volker V Robinson Phillip J PJ McCluskey Adam A
ACS medicinal chemistry letters 20120326 5
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 rep ...[more]
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