Evaluation of antitumor properties of novel saframycin analogs in vitro and in vivo

Novel analogs of (−)-saframycin A are described. The analogs are shown to be potent inhibitors of the in vitro growth of several tumor cells in a broad panel and promising as leads for further optimization. The first in vivo studies in a solid tumor model (HCT-116) reveal potent antitumor activity with associated toxicity of daily administration.

Graphical abstractNovel analogs of (−)-saframycin A are described. Analogs are shown to be potent inhibitors of the in vitro growth of several tumor cells and active antitumor agents in a solid tumor model (HCT-116).Figure optionsDownload full-size imageDownload as PowerPoint slide