Synthesis and screening of novel anthraquinone-quinazoline multitarget hybrids as promising anticancer candidates.

The EGF receptor (EGFR) is overexpressed in multiple epithelial-derived cancers and is considered to be a vital target closely associated with cancer therapy. In this study, a series of novel anthraquinone-quinazoline hybrids targeting several vital sites for cancer therapy were designed and synthesized. Most of the synthesized hybrids demonstrated excellent antiproliferative activity and downregulation of the expression of EGFR. The most promising compound showed the strongest antiproliferation activity; this compound significantly downregulated the expression of p-EGFR protein, induced a remarkable apoptosis effect, promoted the rearrangement of F-actin filaments and destruction of cytoskeleton, induced DNA damage and enhanced radiosensitivity of A549 cells. The novel anthraquinone-quinazoline hybrid emerges as an anticancer drug candidate with promising multitargeted biological activities.