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. 2025 Mar;17(5):513-528.
doi: 10.1080/17568919.2025.2467616. Epub 2025 Mar 3.

Protein profiling uncovers IGF-1R inhibition potential of 3-(2-furoyl)-indole scaffolds in hepatocellular carcinoma

Efficiency Myrsing  1 , H M Chandra Mouli  1   2 , Pallaprolu Nikhil  1 , Deepali  3 , Abhishek Sahu  3 , Anupam Jana  1 , P Ramalingam  1
Affiliations

Protein profiling uncovers IGF-1R inhibition potential of 3-(2-furoyl)-indole scaffolds in hepatocellular carcinoma

Efficiency Myrsing et al. Future Med Chem. 2025 Mar.

Abstract

Aim: This study investigates the anti-proliferative potential and possible molecular mechanisms of 3-(2-furoyl)-indole derivatives against HepG2.

Method: Identified hit compounds (4a, 4b, 4c) using MTT screening, were further investigated for their efficacy and mechanism of action through FACS studies, in-silico molecular docking, molecular dynamics (MD) simulations, and label-free quantitative proteome and ADMET prediction.

Results: Lead compound 4a, showed IC50 of 27 µM against HepG2 cells and a binding score of -8.077 kcal/mol against IGF-1 R (PDB ID: 5XFS) and formed a stable complex 100 ns. Proteomic study revealed significant downregulation of the IGF-1 R downstream signaling molecules and showed minimal toxicity and favorable drug-like properties.

Conclusion: These findings suggest that 4a is a promising IGF-1 R inhibitor and potential drug candidate against drug resistance hepatocellular carcinoma (HCC).

Keywords: 3-(2-furoyl)-indole; HepG2; IGF-1R; hepatocellular carcinoma; label-free proteomics.

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Conflict of interest statement

No potential conflict of interest was reported by the author(s).

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