Inspired by bis-β-carboline alkaloids: Construction and antitumor evaluation of a novel bis-β-carboline scaffold as potent antitumor agents

Bis-β-carboline alkaloids represent an attractive privileged scaffold for discovery of new drugs. Herein, we developed a new synthetic methodology to construct a novel and simplified bis-β-carboline scaffold via “one-pot” condensation-Mannich reaction. Analog 3m displayed potent in-vitro antitumor activity. Mechanism study revealed 3m was a potent both Top1 and Top2 inhibitor, representing a promising lead compound for discovery of new antitumor agents.