Indazole Derivatives: Promising Anti-tumor Agents.

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.