Background: Currently, cancer continues being a dramatically increasing and serious threat to public
health. Although many anti-tumor agents have been developed in recent years, the survival rate of patients is not
satisfactory. The poor prognosis of cancer patients is closely related to the occurrence of drug resistance. Therefore,
it is urgent to develop new anti-tumor agents to make up for the deficiency. Indazoles is an important class
of heterocyclic compounds possessing a variety of biological activities, such as anti-tumor, anti-bacterial, antiinflammatory,
anti-depressant and anti-hypertensive. This review focuses on the recent research advances of
indazole derivatives in the aspect of anti-tumor.
Methods: We have searched the recent literatures about indazole derivatives from the online resources and
databases, such as pubmed, scifinder and google scholar.
Results: In the recent years, many efforts have been taken to develop indazole derivatives as fibroblast growth
factor receptor (FGFR) inhibitors, indoleamine-2,3-dioxygenase1 (IDO1) inhibitors, proviral integration site
MuLV (Pim) kinase inhibitors, aurora kinases inhibitors, Bcr-Abl inhibitors, hypoxia inducible factor-1 (HIF-1)
inhibitors and carbonic anhydrase (CA) inhibitors. Most compounds display good anti-tumor activities.
Conclusion: Developing new anti-cancer agents with new scaffolds and high efficiency is a big challenge for
researchers. Indazole derivatives are a class of important bioactive compounds. Making structural modifications
on active indazole derivatives according to the corresponding structure-activity relationships is of benefit to
obtain more potent anti-cancer leads or clinical drugs. This review will be useful for further development of new
indazole-based derivatives as anti-cancer agents.