Synthesis of novel purpurealidin analogs and evaluation of their effect on the cancer-relevant potassium channel KV10.1.

摘要: In the search for novel anticancer drugs, potassium channel KV10.1 has emerged as an interesting cancer target. Here, we report a new group of inhibitors, namely purpurealidin analogs. These alkaloids are produced by Verongida sponges and known their wide variety bioactivities. this study, describe synthesis characterization 27 Structurally, bromine substituents at central phenyl ring methoxy distal seem to enhance activity on KV10.1. The mechanism action most potent analog 5 was investigated. A shift activation curve more negative potentials apparent inactivation observed. Since inhibitors can be drug lead compounds, effect evaluated cancerous non-cancerous cell lines. Compound showed cytotoxic appeared induce apoptosis in all