Work

Synthesis of Novel Indole Derivatives, Antiproliferative Activity, Apoptosis, and Molecular Docking Studies

Year: 2025

Type: article

Abstract: Novel indole-containing analogs were synthesized via a one-pot, multi-component Passerini reaction and subsequently evaluated for their anticancer activity against HeLa, MCF-7, and A549 cancer cell lines using the MTT assay. Among the synthesized compounds, (2-(cyclohexylamino)-1-(3-fluorophenyl)-2-oxoethyl 2-(1H-indol-3-yl)acetate (4f), which demonstrated the most potent cytotoxic activity, exhibited promising results with IC50 values of 17.71 and 19.92 μM against HeLa and MCF-7 cells, respectively. Flow cytometry analysis confirmed that compound 4f significantly induced apoptosis in HeLa cells in a concentration-dependent manner. Furthermore, molecular docking studies into the active site of the anti-apoptotic protein Bcl-xL indicated that compound 4f binds with good affinity, which is consistent with its considerable efficacy in the in vitro tests.

Source: Acta chimica slovenica

DOI: 10.17344/acsi.2025.9406

Authors: Mahsa Toolabi, Zahra Sabzevari, Zakaria Forouzanfar, Ayyub Mojaddami

Institution: Ahvaz Jundishapur University of Medical Sciences

Language: English

Topic: Multicomponent Synthesis of Heterocycles

Subfield: Organic Chemistry

Field: Chemistry

Domain: Physical Sciences

SDG: Good health and well-being

Open Access status: diamond

Funder: Ahvaz Jundishapur University of Medical Sciences