850152-91-9Relevant academic research and scientific papers
Design, synthesis and bioactivity evaluation of fisetin derivatives as potential anti-inflammatory agents against LPS-induced acute lung injury
Wang, Xiemin,Yang, Jun,Ding, Bingyu,Chen, Pan,Xu, Zhengwei,Zhao, Yunxi,Chen, Pengqin,Chattipakorn, Nipon,Liang, Guang,Wu, Di,Tang, Qidong
, (2021/10/12)
Acute lung injury (ALI) refers to a common and life-threatening disease attributed to inflammation. However, effective drug treatments have been rare for ALI. Natural products have been considered as a vital source of drug discovery which indicates that it's a workable method to find new anti-inflammatory drugs in natural products. Inspired by the various biological activities of fisetin, we reported the design and synthesis of a series of fisetin derivatives which were also evaluated for their anti-inflammatory activities in J774A.1 macrophages. Most of the obtain derivatives could effectively inhibit the release of IL-6 and TNF-α in vitro experiments without cytotoxicity. The most promising compound 5b exhibited significant in vivo anti-inflammatory activity in the model of LPS-induced ALI in mice. On the whole, this study could provide novel candidates for the treatment of ALI.
Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease
Bai, Ping,Wang, Keren,Zhang, Pengfei,Shi, Jian,Cheng, Xinfeng,Zhang, Qi,Zheng, Cheng,Cheng, Yao,Yang, Jian,Lu, Xiaoxia,Sang, Zhipei
, (2019/10/02)
A series of novel chalcone-O-alkylamine derivatives were designed, synthesized and evaluated as multifunctional anti-Alzheimer's disease agents. Based on the experimental results, compound 23c exhibited good inhibitory potency on both acetylcholinesterase
Design, synthesis and biological evaluation of 2-acetyl-5-O-(amino-alkyl)phenol derivatives as multifunctional agents for the treatment of Alzheimer's disease
Sang, Zhipei,Wang, Keren,Wang, Huifang,Wang, Huijuan,Ma, Qianwen,Han, Xue,Ye, Mengyao,Yu, Lintao,Liu, Wenmin
, p. 5046 - 5052 (2017/10/20)
A series of 2-acetyl-5-O-(amino-alkyl)phenol derivatives was designed, synthesized and evaluated as multi-function inhibitors for the treatment of Alzheimer's disease (AD). The results revealed that compound TM-3 indicated selective AChE inhibitory potenc
Homopterocarpanes as bridged triarylethylene analogues: Synthesis and antagonistic effects in human MCF-7 breast cancer cells
Rampa, Angela,Bisi, Alessandra,Belluti, Federica,Gobbi, Silvia,Piazzi, Lorna,Valenti, Piero,Zampiron, Antonella,Caputo, Anna,Varani, Katia,Borea, Pier Andrea,Carrara, Maria
, p. 135 - 147 (2007/10/03)
A series of new compounds structurally derived from 6a,12a-dihydro-6H,7H- [1]-benzopyran-[4,3-b]-benzopyran (homopterocarpane) was efficiently synthesized by reduction of the corresponding pyrilium salts obtained by treatment of selected flavanones and aldehydes with anhydrous HClO4. Cytotoxic effects on the human breast cancer cell line MCF-7 and antiestrogenic activity (only for compounds which resulted more active than tamoxifen (TAM)) on MCF-7 cells stimulated by 17β-estradiol were evaluated. In vivo antiestrogenic activity and the relative binding affinity were also assessed. Some of the new compounds (4c, 4h, 4i and 4l) showed a biological activity in the micromolar range, and were more potent than TAM taken as the reference.
