Inhibition of dynamin mediated endocytosis by the dynoles--synthesis and functional activity of a family of indoles.

@article{Hill2009InhibitionOD,
  title={Inhibition of dynamin mediated endocytosis by the dynoles--synthesis and functional activity of a family of indoles.},
  author={Timothy A. Hill and Christopher P Gordon and Andrew B. McGeachie and Barbara Venn-Brown and Luke R Odell and Ngoc Diep Chau and Annie Quan and Anna Mariana and Jennette A Sakoff and Megan Chircop and Phillip J Robinson and Adam McCluskey},
  journal={Journal of medicinal chemistry},
  year={2009},
  volume={52 12},
  pages={3762-73}
}
Screening identified two bisindolylmaleimides as 100 microM inhibitors of the GTPase activity of dynamin I. Focused library approaches allowed development of indole-based dynamin inhibitors called dynoles. 100-Fold in vitro enhancement of potency was noted with the best inhibitor, 2-cyano-3-(1-(2-(dimethylamino)ethyl)-1H-indol-3-yl)-N-octylacrylamide… CONTINUE READING