Discovery of cytotoxic indolo[1,2-<i>c</i>]quinazoline derivatives through scaffold-based design.

ABSTRACT: Indolo[1,2-c]quinazoline derivatives have emerged as promising chemotype in drug discovery due to their versatile biological activities, including antimicrobial and antiviral properties. In this study, we report the design, synthesis, and biological evaluation of novel indolo[1,2-c]quinazoline derivatives, with a particular focus on their antiproliferative potential against human cancer cells. We introduced structural modifications at positions 5, 6, and 12 of the indolo[1,2-c]quinazoline core to explore the structure-activity relationships and enhance cytotoxicity. Our results highlight that 12-aminomethyl derivatives exhibited notable cytotoxicity against tumor cell lines, with the highest activity observed for compound 9c, which showed significant selectivity

SUBMITTER: Khabarov DV 

PROVIDER: S-EPMC12536455 | biostudies-literature | 2025

REPOSITORIES: biostudies-literature