Azaindole framework is an important part of several biologically active natural and synthetic organic molecules; and several FDA approved drugs for various diseases. In contrast to 4-, 5, and 6-azindoles, 7-azaindole derivatives have attracted most attention due to their remarkable physicochemical and pharmacological properties. Azaindoles are often used as the bioisoteres of indoles to improve the activities in anticancer drug discovery. So far, many 7-azazinole derivatives have been reported as potent anticancer agents, and some have been used in clinics. This chapter covers the recent progress in the field of anticancer drug development employing a 7-azaindole scaffold.