The incidence and mortality of cancer continue to grow since the current medical treatments
often fail to produce a complete and durable tumor response and ultimately give rise to therapy
resistance and tumor relapse. Heterocycles with potential therapeutic values are of great pharmacological
importance, and among them, indazole moiety is a privileged structure in medicinal chemistry.
Indazole compounds possess potential anticancer activity, and indazole-based agents such as, axitinib,
lonidamine and pazopanib have already been employed for cancer therapy, demonstrating indazole
compounds as useful templates for the development of novel anticancer agents. The aim of this review
is to present the main aspects of exploring anticancer properties, such as the structural modifications,
the structure-activity relationship and mechanisms of action, making an effort to highlight the
importance and therapeutic potential of the indazole compounds in the present anticancer agents.