Synthesis and cytotoxic activity evaluation of indole carbohydrazide derivatives

Abstract

Indole derivatives are considered to have great potential in the synthesis and development of cancer drugs. The main objective of this study was to synthesise some indole carbohydrazide derivatives and test their cytotoxicity on human cancer cell lines. A series of indole carbohydrazide derivatives was synthesised by the basic condensation reaction. The chemical structure of these compounds was elucidated by ¹H-NMR, ¹³C-NMR, and MS spectral analysis. The in vitro cytotoxic activities of all synthesised compounds against human colon cancer cells (HT-29) were evaluated by the SRB assay. The results showed that compounds II_a , II_b , II_c, and II_f exhibited activity against the tested cell lines with IC₅₀ values ranging from 1.72 to 48.85 µM. Especially, the compound IIa displayed the most potent anticancer activity against HT-29 cells with IC₅₀=1.72±0.29 µM. The study results suggest important information about the synthesis and development of new cancer drugs from the indole carbohydrazide framework, contributing to the orientation of future comprehensive studies in the search for cytotoxic compounds against cancer cells from derivatives bearing the indole carbohydrazide scaffold using chemical synthesis methods.