title: The Rhodadyns, a New Class of Small Molecule Inhibitors of Dynamin GTPase Activity.
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.
authors.affiliation: Chemistry, The University of Newcastle , University Drive, Callaghan, NSW 2308, Australia.
authors.forename: Mark J
authors.initials: MJ
authors.lastname: Robertson
authors.affiliation: Chemistry, The University of Newcastle , University Drive, Callaghan, NSW 2308, Australia.
authors.forename: Gordana
authors.initials: G
authors.lastname: Hadzic
authors.affiliation: Chemistry, The University of Newcastle , University Drive, Callaghan, NSW 2308, Australia.
authors.forename: Joseph
authors.initials: J
authors.lastname: Ambrus
authors.affiliation: Chemistry, The University of Newcastle , University Drive, Callaghan, NSW 2308, Australia.
authors.forename: D Yuri
authors.initials: DY
authors.lastname: Pomè
authors.affiliation: Chemistry, The University of Newcastle , University Drive, Callaghan, NSW 2308, Australia.
authors.forename: Emily
authors.initials: E
authors.lastname: Hyde
authors.affiliation: Cell Signalling Unit, Children's Medical Research Institute, The University of Sydney , Sydney, NSW 2145, Australia.
authors.forename: Ainslie
authors.initials: A
authors.lastname: Whiting
authors.affiliation: Cell Signalling Unit, Children's Medical Research Institute, The University of Sydney , Sydney, NSW 2145, Australia.
authors.forename: Anna
authors.initials: A
authors.lastname: Mariana
authors.affiliation: Leibniz Institut für Molekulare Pharmakologie & Freie Universität Berlin , 13125 Berlin, Germany.
authors.forename: Lisa
authors.initials: L
authors.lastname: von Kleist
authors.affiliation: Cell Signalling Unit, Children's Medical Research Institute, The University of Sydney , Sydney, NSW 2145, Australia.
authors.forename: Ngoc
authors.initials: N
authors.lastname: Chau
authors.affiliation: Leibniz Institut für Molekulare Pharmakologie & Freie Universität Berlin , 13125 Berlin, Germany.
authors.forename: Volker
authors.initials: V
authors.lastname: Haucke
authors.affiliation: Cell Signalling Unit, Children's Medical Research Institute, The University of Sydney , Sydney, NSW 2145, Australia.
authors.forename: Phillip J
authors.initials: PJ
authors.lastname: Robinson
authors.affiliation: Chemistry, The University of Newcastle , University Drive, Callaghan, NSW 2308, Australia.
authors.forename: Adam
authors.initials: A
authors.lastname: McCluskey
keywords: Knoevengal condensation; dynamin inhibition; rhodanine