875242-62-9Relevant academic research and scientific papers
Apoptosis-inducing effects and growth inhibitory of a novel chalcone, in human hepatic cancer cells and lung cancer cells
Dong, Naiwei,Liu, Xin,Zhao, Tong,Wang, Lei,Li, Huimin,Zhang, Shuqian,Li, Xia,Bai, Xue,Zhang, Yong,Yang, Baofeng
, p. 195 - 203 (2018)
Apoptosis is an important biological phenomenon, which affects many diseases, such as cancer and Alzheimer's disease. In the present study, we observed that chalcone 9X, an aromatic ketone, induced apoptosis of human hepatic and lung cancer cells and inhi
Discovery of CAPE derivatives as dual EGFR and CSK inhibitors with anticancer activity in a murine model of hepatocellular carcinoma
Liu, Xiaoyu,Du, Qianqian,Tian, Caiping,Tang, Mei,Jiang, Yingjun,Wang, Yong,Cao, Yang,Wang, Zhe,Wang, Zhenwei,Yang, Jing,Li, Yan,Jiao, Xiaozhen,Xie, Ping
, (2020/12/25)
Caffeic acid phenethyl ester (CAPE), a bioactive component extracted from propolis of honeybee hives, can inhibit hepatocellular carcinoma (HCC). In order to explore more stable CAPE derivatives, 25 compounds were designed, synthesized, and pharmacologically assessed in vitro and in vivo as anti-tumor agents in HCC. Compounds 8d, 8f, 8l, 8j, and 8k showed favorable antiproliferative activity than other compounds including CAPE in the HCC cell lines. Based on the result of QTRP (Quantitative Thiol Reactivity Profiling), epidermal growth factor receptor (EGFR) and C-terminal Src kinase (CSK) were supposed to the targets of 8f, which was confirmed by binding mode analysis. Furthermore, compounds 8f, 8l, 8j, 8k, 8g, and 8h showed potent inhibitory effects against both CSK and EGFR than other derivatives in an ADP-Glo kinase assay. The representative compound, 8f, potently inhibited various tumor growth in murine model including murine hepatocellular carcinoma H22, meanwhile downregulating the EGFR/AKT pathway and enhancing T cell proliferation through inhibition of CSK. Metabolic stability in vitro suggested 8f and 8k were more stable in mouse plasma than CAPE and susceptible to metabolism in liver microsomes. The overall excellent profile of compound 8f makes it a potential candidate for further preclinical investigation.
Phenethyl caffeate derivative, preparation method, pharmaceutical composition and application thereof
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Paragraph 0150-0154; 0163-0164, (2021/03/05)
The invention discloses a phenethyl caffeate derivative, a preparation method, a pharmaceutical composition and application thereof. Specifically, the invention relates to a compound shown as formula(I) or an isomer and pharmaceutically acceptable salt th
4 ’ - Hydroxyl -3 ’ - methoxy chalcone derivatives. Preparation method and application thereof in anti-tumor
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Paragraph 0027-0034, (2020/12/30)
The invention discloses 4'-hydroxy-3'-methoxychalcone derivatives, a preparation method thereof and an application in tumor resistance. The chemical structural formula of the 4'-hydroxy-3'-methoxychalcone derivatives is shown in the following formula I in
Inhibitory effects of chalcone glycosides isolated from Brassica rapa L. 'hidabeni' and their synthetic derivatives on LPS-induced NO production in microglia
Hara, Hirokazu,Nakamura, Yoko,Ninomiya, Masayuki,Mochizuki, Ryosuke,Kamiya, Tetsuro,Aizenman, Elias,Koketsu, Mamoru,Adachi, Tetsuo
experimental part, p. 5559 - 5568 (2011/10/17)
Activation of microglia induces the production of various inflammatory mediators including nitric oxide (NO), leading to neurodegeneration in many central nervous system diseases. In this study, we examined the effects of chalcone glycosides isolated from
