In 1977 an unknown natural product was isolated from Streptomyces staurosporeus by Omura et al. during a search for new alkaloids present in actinomycetes and was given the name AM-2282. Later, the structure of AM-2282 was elucidated by single crystal X-ray analysis and renamed as staurosporine. It has been published that staurosporine and its analogues display strong inhibitory effect against a variety of kinases and a number of biological properties such as antifungal, antibacterial, and immunosuppressive activities. Despite strong inhibitory activity of staurosporine, a very high level of cross-reactivity makes it impossible to use staurosporine as a therapeutic agent. In the course of searching for other staurosporine-related compounds, a number of staurosporine analogues have been isolated from different microorganisms. In addition, a number of staurosporine analogues have been synthesized to improve the poor selectivity and target specificity of staurosporine which limited its clinical effectiveness. The review addresses staurosporine analogues from both microbial and synthetic sources and their biological activities.