Tuning Scaffold Properties of New 1,4-Substituted Pyrrolo[3,2-c]quinoline Derivatives Endowed with Anticancer Potential, New Biological and In Silico Insights

    December 2025 in “ Biomolecules
    Francesco Mingoia, Caterina Di Sano, Claudia D’Anna, Marco Fazzari, Alessia Bono, Gabriele La Monica, Annamaria Martorana, Antonino Lauria
    TLDR Compound 7p shows strong potential as an anticancer agent.
    A new series of pyrrolo[3,2-c]quinoline derivatives was synthesized to enhance antiproliferative activity, focusing on modifications to the benzodioxole moiety. Through NCI antiproliferative screening and MTS-based assays, compound 7p was identified as a promising hit, showing cytotoxic activity in the low micromolar range against MCF-7 and HeLa cells. Additional biological evaluations, such as apoptosis induction and clonogenic tests, supported its anticancer potential. In silico docking revealed a multi-target profile, indicating potential for rational polypharmacology and guiding further lead optimization for enhanced anticancer activity.
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