Synthesis and biological evaluation of indazole derivatives as anti-cancer agents

Abstract

One of the synthesized indazole derivatives, 2f, displayed inhibitory activities against proliferation, migration and invasion of breast cancer cell line 4T1, with the potential of inducing cell apoptosis, and suppressing tumor growth in vivo.

A review on synthetic strategy, molecular pharmacology of indazole derivatives, and their future perspective

“…A (pyridine‐2‐yl)piperazine clubbed with indazole derivative ( 191 ) had shown excellent in‐vitro antiproliferative activity against 4T1 (mouse breast cancer) and MCF‐7 cell line with IC 50 values of 0.23 and 0.34 µM, respectively. Wei et al (2021) suggested that compound 191 (Figure 20) might induce mitochondrial apoptotic pathway via caspase‐3 dependent manner using annexin V‐FITC/PI flow cytometry assay and western blot analysis. In 4T1‐tumor‐bearing female BalB/c mice, it was tested in‐vivo for anticancer activity at doses of 12.5 and 25 mg/kg once a day, which suggested dose‐dependent suppression of tumor volume with no obvious and remarkable side effect (Wei et al, 2021).…”

“…Wei et al (2021) suggested that compound 191 (Figure 20) might induce mitochondrial apoptotic pathway via caspase‐3 dependent manner using annexin V‐FITC/PI flow cytometry assay and western blot analysis. In 4T1‐tumor‐bearing female BalB/c mice, it was tested in‐vivo for anticancer activity at doses of 12.5 and 25 mg/kg once a day, which suggested dose‐dependent suppression of tumor volume with no obvious and remarkable side effect (Wei et al, 2021).…”

“…Dual IDO1 and TDO inhibitory activity increase if the benzo‐thiazole moiety or a cyano group is linked with the 4‐amine of indazole ( 195 ); while selectivity toward TDO increases when 2‐amino thiazole is replaced with benzothiazole in compound 195 (L. Yang et al, 2019). sixth positional pyridine substitution in indazole forms pyridyl‐indazole derivatives ( 191 ) which dramatically increases anticancer potency when linked with 3,4‐dimethoxyphenyl moiety via vinyl or ethyl substitution at third position of indazole (Wei et al, 2021). Substituents like 4‐hydroxy‐1‐phenylbut‐2‐yn‐1‐one in the fifth position of 3‐benzothiazolyl indazole derivative ( 189 ) increase anticancer activity against the number of cell lines (Sandeep Reddy et al, 2018).…”

“…Pyridine-2-yl-piperazine clubbed indazole derivative with anticancer activityA (pyridine-2-yl)piperazine clubbed with indazole derivative (191) had shown excellent in-vitro antiproliferative activity against 4T1 (mouse breast cancer) and MCF-7 cell line with IC 50 values of 0.23 and 0.34 µM, respectively Wei et al (2021). suggested that compound 191 (Figure20) might induce mitochondrial apoptotic pathway via caspase-3 dependent manner using annexin V-FITC/PI flow cytometry assay and western blot analysis.…”

Study of the Addition Mechanism of 1H-Indazole and Its 4-, 5-, 6-, and 7-Nitro Derivatives to Formaldehyde in Aqueous Hydrochloric Acid Solutions

“…A search in different databases shows that the chemistry of indazoles is a very active field; the numbers of items are 11 723 (Scifinder), 5142 (ScienceDirect), and 4448 (Web of Science); and most of the papers and patents deal with biological applications. − Other applications (corrosion inhibitors) and synthetic methods are less reported, and the last place is occupied by indazole reactivity.…”