The importance of indole and azaindole scaffold in the development of antitumor agents.

With some indoles and azaindoles being successfully developed as anticancer drugs, the design and synthesis of indole and azaindole derivatives with remarkable antitumor activity has received increasing attention and significant progress has been made. This paper reviews the recent progress in the study of tumorigenesis, mechanism of actions and structure activity relationships about anticancer indole and azindole derivatives. Combining structure activity relationships and molecular targets-related knowledge, this review will help researchers design more effective, safe and cost-effective anticancer indoles and azindoles agents.