Synthesis and therapeutic evaluation of pyridyl based novel mTOR inhibitors

A series of novel cyanopyridyl based molecules (1–14) were designed, synthesized and probed for inhibition of mammalian target of rapamycin (mTOR) activity. Compound 14 was found to be a potent inhibitor of mTOR activity as assessed by enzyme-linked immunoassays and Western blot analysis. Most importantly, systemic application (intraperitoneal; ip) of compound 14 significantly suppressed macroscopic and histological abnormalities associated with chemically-induced murine colitis.

Graphical abstractSystemic application of compound 14, a novel mTOR inhibitor, significantly suppresses macroscopic and histologic abnormalities associated with chemically-induced murine ulcerative colitis.Figure optionsDownload full-size imageDownload as PowerPoint slide