A new study from Singh et al. at Babasaheb Bhimrao Ambedkar University (India) presents the synthesis, characterization and evaluation of indole-fused benzooxazepines. This new class of compounds was then tested for anticancer activity against hepatocellular carcinoma.
The compounds comprise an indole moiety directly attached to benzooxazepine with a relatively flexible six-membered hydrophobic ring in a single-molecular framework.
In vitro testing on Hep-G2 cancer cells, plus computational and ADMET study on cancer-related targets including IL-2, IL-6, COX-2 Caspase-3 and Caspase-8, highlighted 5 compounds as of interest for further, in vivo study. The in vitro testing suggested that substitutions with more electronegative groups at phenyl ring directly attached with indole-fused benzooxazepine generally elicited enhanced cytotoxic potential.
The full manuscript is open access and available here.
Indole-fused benzooxazepines: a new structural class of anticancer agents
Ashok K Singh, Vinit Raj, Amit Rai, Amit K Keshari, Sudipta Saha
Future Science OA, FSO168, doi:10.4155/fsoa-2016-0079 (2016).