Work

Discovery of Primaquine–Indole Carboxamides with Cancer-Cell-Selective Antiproliferative Activity

Year: 2025

Type: article

Abstract: Indole carboxylic acids are endogenous tryptophan metabolites that have demonstrated a variety of bioactivities, including anticancer effects. Specifically, indole acetic acid (IAA) elicits anticancer activity when combined with ultraviolet B or reactive oxygen species (ROS) generators. Primaquine (PQ) is an approved drug which elicits antimalarial activity through ROS generation. We investigated the effects of ICA, IAA, PQ, their combination and PQ–indole carboxamide conjugates on the viability of selected cancer cell lines. We identified PQ–indole carboxamide 2 which elicited more potent antiproliferative effects than PQ and ICA/PQ combination. Our data revealed that compound 2 derived a significant part of its antiproliferative effect from ROS generation.

Source: Molecules

DOI: 10.3390/molecules30193988

Authors: Benjamin H. Peer, Jeremiah O. Olugbami, Dipak T. Walunj, Adegboyega K. Oyelere

Institution: Georgia Institute of Technology

Language: English

Topic: Bioactive Compounds and Antitumor Agents

Subfield: Toxicology

Field: Pharmacology, Toxicology and Pharmaceutics

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: gold

Estimated APC paid: $3,258