83649-26-7Relevant academic research and scientific papers
Discovery of chalcone-modified estradiol analogs as antitumour agents that Inhibit tumour angiogenesis and epithelial to mesenchymal transition
Wang, Cong,Li, Leilei,Fu, Dongyang,Qin, Tiantian,Ran, Yange,Xu, Feng,Du, Xinrui,Gao, Haiying,Sun, Shuaijun,Yang, Tengjiao,Zhang, Xueyan,Huo, Junfeng,Zhao, Wen,Zhang, Zhenzhong,Shi, Xiufang
, p. 135 - 148 (2019/05/17)
Angiogenesis plays an essential role in tumourigenesis and tumour progression, and anti-angiogenesis therapies have shown promising antitumour effects in solid tumours. 2-Methoxyestradiol (2ME2), an endogenous metabolite of estradiol, has been regarded as a potential antitumour agent mainly targeting angiogenesis. Here we synthesized a novel series of chalcones based on 2-methoxyestradiol and evaluated their potential activities against tumours. Compound 11e was demonstrated to have potent antiangiogenic activity. Further studies showed that 11e suppressed tumour growth in human breast cancer (MCF-7)xenograft models without obvious side effects. Evaluation of the mechanism revealed that 11e targeted the epithelial to mesenchymal transition (EMT)process in MCF-7 cells and inhibited HUVEC migration and then contributed to hindrance of angiogenesis. Thus, 11e may be a promising antitumour agent with excellent efficacy and low toxicity.
For female steroid nucleus to 2 bit or 16 substituted chalcone derivative and its preparation and use
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Paragraph 0100; 0102, (2017/08/26)
The invention belongs to the field of medicinal chemicals, and relates to a 2/16-site-substituted chalcone derivative taking estrogen as a mother nucleus and a preparation method and application of the derivative. The preparation method comprises the following step: combining chalcone structural fragments on an estrogen body in parallel, thereby keeping or improving the activity of anti-tumor cells and inhibiting activity of tumor cell angiogenesis. The structural formula of the 2/16-site-substituted chalcone derivative is as shown in the specification. The in-vitro anti-tumor cell proliferation activity test and the chick embryo allantois test show that the derivative has certain anti-tumor cell proliferation activity and inhibiting activity of tumor cell angiogenesis; and the dose-effect relationship study shows that the tumor cell inhibition function of the derivative is prior to that of 2-methoxy estradiol with broad-spectrum anti-tumor activity, and moreover the half-life period can be prolonged.
Synthesis and antimitotic activity of novel 2-methoxyestradiol analogs. Part III
Rao, Pemmaraju N.,Cessac, James W.,Boyd, James W.,Hanson, Arthur D.,Shah, Jamshed
, p. 171 - 183 (2008/03/18)
The syntheses and antimitotic activity of several novel analogs of 2-methoxyestradiol are described. Structural modifications include ring-D homologation, aromatization of the six-membered ring-D to a chrysine type molecule, and introduction of unsaturation in five-membered ring-D along with substitution of alkyl and ethynyl groups for the 17β-hydroxy function. Of nine analogs synthesized, five have demonstrated superior antiproliferative activities compared to 2-methoxyestradiol.
2-ALKOXYESTRADIOL ANALOGS AND PHARMACEUTICAL PREPARATIONS
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Page/Page column 38, (2009/01/20)
Novel 2-alkoxyestradiol analogs, pharmaceutical compositions and methods of treatment of proliferative and angiogenesis associated conditions are disclosed.
