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

Synthesis and Anticancer Properties of Oxazepines Related to Azaisoerianin and IsoCoQuinesSynthesis and Anticancer Properties of Oxazepines Related to Azaisoerianin and IsoCoQuines. ChemMedChem. 2020 Jun 02;: Authors: Provot O, Khelifi I, Pecnard S, Bernadat G, Bignon J, Levaique H, Dubois J, Alami M Abstract : In this article, we reported the synthesis and the biological properties of a series of novel oxazepines 1 endowed with antitumor properties. Among them, we found that oxazepin-9-ol 1f and ester derivative 1j displayed a nanomolar level of cytotoxicity. Remarkably, oxazepin-9-ol 1g having in structure a 2-cyanoquinoline linked on C4 to a benzo[b][1,4]oxazepine ring was found to be the lead molecule in this series displaying a (sub)nanomolar cytotoxicity level against five human cancer cell lines (HCT116, U87, A549, MCF7 and K562). Moreover, oxazepin-9-ol 1g inhibited the tubulin assembly with an IC 50 value of 1 mM and totally arrested the cellular cycle in the G2/M phase at a low concentration of 5 nM in HCT116 and K562 cells. PMID: 32485077 [PubMed - as supplied by publisher]
Source: ChemMedChem - Category: Chemistry Authors: Tags: ChemMedChem Source Type: research