- Title
- The rhodadyns, a new class of small molecule inhibitors of dynamin GTPase activity
- Creator
- Robertson, Mark J.; Hadzic, Gordana; Robinson, Phillip J.; McCluskey, Adam; Ambrus, Joseph; Pomé, D. Yuri; Hyde, Emily; Whiting, Ainslie; Mariana, Anna; von Keist, Lisa; Chau, Ngoc; Haucke, Volker
- Relation
- ACS Medicinal Chemistry Letters Vol. 3, Issue 5, p. 352-356
- Publisher Link
- http://dx.doi.org/10.1021/ml200284s
- Publisher
- American Chemical Society
- Resource Type
- journal article
- Date
- 2012
- Description
- 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.
- Subject
- dynamin inhibition; knoevengal condensation; rhodanine
- Identifier
- http://hdl.handle.net/1959.13/1309005
- Identifier
- uon:21743
- Identifier
- ISSN:1948-5875
- Rights
- This document is the Accepted Manuscript version of a Published Work that appeared in final form in ACS Medicinal Chemistry Letters, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see http://pubs.acs.org/page/policy/articlesonrequest/index.html.
- Language
- eng
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