The Synthesis and Biological Evaluation of Aloe-Emodin-Coumarin Hybrids as Potential Antitumor Agents

Author:

Shang Hai,Hu Yue,Li Jingrong,Li LingyuORCID,Tian Yu,Li Xiaoxue,Wu Qi,Zou ZhongmeiORCID

Abstract

A series of novel aloe-emodin–coumarin hybrids were designed and synthesized. The antitumor activity of these derivatives was evaluated against five human tumor cell lines (A549, SGC-7901, HepG2, MCF-7 and HCT-8). Some of the synthesized compounds exhibited moderate to good activity against one or more cell lines. Particularly, compound 5d exhibited more potent antiproliferative activity than the reference drug etoposide against all tested tumor cell lines, indicating that it had a broad spectrum of antitumor activity and that it may provide a promising lead compound for further development as an antitumor agent by structural modification. Furthermore, the structure–activity relationship study of the synthesized compounds was also performed.

Funder

CAMS Innovation Fund for Medical Sciences

Publisher

MDPI AG

Subject

Chemistry (miscellaneous),Analytical Chemistry,Organic Chemistry,Physical and Theoretical Chemistry,Molecular Medicine,Drug Discovery,Pharmaceutical Science

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