Abstract
Abstract— A series of indolylpyridopyrimidine derivatives were designed, synthesized, and tested for their in vitro cytotoxic activity using the SRB assay method. The antiproliferative activities of the new compounds were tested against HepG-2 and MCF-7 human cancer cell lines. All candidates exhibited more powerful activity against MCF-7 with IC50 values ranging from 7.5 ± 0.5 to 10.0 ± 1.1 μM compared to the positive control, Doxorubicin. On the other hand compounds (VIIId), (Vc), and (VIIIb), had similar activities on HepG-2; the other compounds had slightly fewer activities relative to the positive control doxorubicin. The results of the molecular docking demonstrated that the biological and theoretical concepts are well-computable, adding to the research’s value. As a result, this study provides a framework for additional research towards indolylpyridopyrimidine derivatives as antiproliferative drugs.