The Rhodadyns, a New Class of Small Molecule Inhibitors of Dynamin GTPase Activity

[摘要]：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 mu M, 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 mu M, respectively. These compounds are equipotent with the best reported in-cell dynamin inhibitors.

[全文传递流程]：

一般上传文献全文的时限在1个工作日内