Synthesis and Anticancer Properties of Oxazepines Related to Azaisoerianin and IsoCoQuinesSynthesis and Anticancer Properties of Oxazepines Related to Azaisoerianin and IsoCoQuines.

In this article, we report the synthesis and biological properties of a series of novel oxazepines related to isoCA-4 having significant antitumor properties. Among them, three oxazepin-9-ol derivatives display a nanomolar or a (sub)nanomolar cytotoxicity level against five human cancer cell lines (HCT116, U87, A549, MCF7 and K562). It was demonstrated that the lead compound in this series inhibits tubulin assembly with an IC50 value of 1 M and totally arrested the cellular cycle in the G2/M phase at a low concentration of 5 nM in HCT116 and K562 cells. Molecular modelling studies perfectly corroborates these promising results.