50264-80-7

Upstream product

• 4498-67-3 1H-Indazole-3-carboxylic acid 
• 104-83-6 1-Chloro-4-(chloromethyl)benzene 
• 43120-28-1 methyl 1H-indazole-3-carboxylate 

Downstream Products

• 50264-86-3 1-(4-Chlorophenyl)-methyl-1H-indazole-3-carboxylic acid 

Relevant academic research and scientific papers

Novel potent HIF-1 inhibitors for the prevention of tumor metastasis: discovery and optimization of 3-aryl-5-indazole-1,2,4-oxadiazole derivatives

Hypoxia inducible factor-1 (HIF-1) is the key transcription factor of cellular response to hypoxia and plays a critical role in tumor metastasis. We describe here the discovery and a structure-activity relationship study of a series of 3-aryl-5-indazole-1,2,4-oxadiazole derivatives as novel HIF-1 inhibitors. The two most promising compounds 4g and 4h inhibit HIF-1 transcription with IC50 values of 0.62 and 0.55 μM in vitro, respectively, and they exhibit more efficient HIF-1 inhibition in xenograft tumors than YC-1, a potential anticancer drug targeting HIF-1. In addition, they also remarkably prevent the hypoxia-driven migration of SKOV3 cells in vitro and tumor metastasis in vivo. Further investigation of the mechanism revealed that the two inhibitors could decrease HIF-1α and VEGF expression. These results suggest that our newly synthesized HIF-1 inhibitors 4g and 4h are potential therapeutic agents with which to treat tumor metastasis.

Indazole-oxadiazole derivative, medicinal composition containing derivative, and application of derivative in tumor prevention

The invention discloses an indazole-oxadiazole derivative with the structure represented by general formula a shown in the description, or a pharmaceutically acceptable salt or solvate thereof. In the formula, X is O or N, Y is N, Z is N or O, and all groups are as defined in the description. The invention also discloses a medicinal composition adopting the derivative as an active component, and a use of the derivative. Compounds synthesized in the invention have an HIF-1 inhibition effect, and most of the compounds have a substantial HIF-1 inhibition effect, have strong in-vivo and in-vitro anti-HIF-1 effect on human colorectal carcinoma cell strains (HCT116) and other tumor cell strains, and can be used for treating tumor diseases.