期刊
FUTURE MEDICINAL CHEMISTRY
卷 12, 期 2, 页码 111-126出版社
FUTURE SCI LTD
DOI: 10.4155/fmc-2019-0230
关键词
anthraquinone; anticancer; hybrid compounds; multitarget biological profiling; quinazoline
资金
- National Natural Science Foundation of China [81460561, 81360502]
- Guangxi Natural Science Foundation [2014GXNSFAA118225, 2018GXNSFAA281064]
- Program of Key Laboratory of High-Incidence-Tumor Prevention and Treatment (Guangxi Medical University)
- Ministry of Education, China [GKE2019-23]
Aim: 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. Methodology & results: Most of the synthesized hybrids demonstrated excellent antiproliferative activity and downregulation of the expression of EGFR. The most promising compound 7d 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. Conclusion: The novel anthraquinone-quinazoline hybrid 7d emerges as an anticancer drug candidate with promising multitargeted biological activities.
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