The Anticancer Activity of Indazole Compounds: A Mini Review

Abstract

: 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 privileged struc-ture in medicinal chemistry. Indazole compounds possess potential anticancer activity, and the indazole-based agents Ax-itinib, Lonidamine and Pazopanib have already been applied for cancer therapy, demonstrating indazole compounds are 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 potentials of the indazole compounds in the present anticancer agents.

Quantitative and Qualitative Analysis of the Anti-Proliferative Potential of the Pyrazole Scaffold in the Design of Anticancer Agents

“…There are many reviews that present and demonstrate the anticancer potential of the pyrazole ring, unfused or fused in structures like indazole or pyrazolopyrimidines, but these works present only on the active derivatives [ 32 , 33 , 34 , 35 , 36 , 37 , 38 ]. The researchers tend to publish only works with positive results in order to maximize their scientific impact.…”

Research and development ofN,N′-diarylureas as anti-tumor agents

“…29 Nitrogen-containing heterocycles, especially the structurally diverse indolazole groups, have prompted a great deal of research due to their diverse biological activities, aiming at their synthetic routes and mechanisms of activity. [30][31][32][33] Due to the outstanding biological activities of benzopyrazole and diarylurea structures in drug development, many benzopyrazole-containing diarylureas have been designed and synthesized in recent years for the screening of anti-tumor drug candidates. Inspired by the chemical structure of sorafenib, Li et al designed and synthesized a series of diarylureas containing indolazole or azaindazole groups (Fig.…”

Potentials and future perspectives of multi-target drugs in cancer treatment: the next generation anti-cancer agents

“…This antiangiogenic drug improved the overall survival of patients with head and neck squamous cell carcinoma [ 136 ]. The common expected side effects of this indazole-based agent are hypertension (16%), fatigue (11%), and diarrhea (11%) [ 137 , 138 ]. Another point to be considered is to monitor proteinuria before initiation and periodically during treatment.…”