101-18-8Relevant articles and documents
A survey on the reactivity of phenyliodonium ylide of 2-hydroxy-1,4- naphthoquinone with amino compounds
Spagou, Konstantina,Malamidou-Xenikaki, Elizabeth,Spyroudis, Spyros
, p. 226 - 237 (2005)
The phenyliodonium ylide of 2-hydroxy-1,4-naphthoquinone reacts with aminoesters, ureas, aminoalcohols and aminophenols in refluxing dichloromethane to afford good yields of indanedione 2-carboxamido compounds, that in solution exist in an enol-amide form. The same reactants in a copper-catalyzed reaction afford mainly the corresponding N-arylo compounds. Arylhydrazines are mainly oxidized by the ylide and arylation occurs only in a low yield.
Discovery of 4-(3,5-dimethoxy-4-(((4-methoxyphenethyl)amino)methyl)phenoxy)-N-phenylaniline as a novel c-myc inhibitor against colorectal cancer in vitro and in vivo
Cao, Chaoguo,Lan, Suke,Li, Rui,Liu, Yuanyuan,Luo, Dan,Luo, Meng,Ma, Xinyu,Shan, Huifang,Yang, Jie,Yu, Su,Zhong, Xinxin
, (2020)
Proto-oncogene c-Myc plays an essential role in the development of colorectal cancer (CRC), since downregulation of c-Myc inhibits intestinal polyposis, which is the most cardinal pathological change in the development of CRC. Herein, a series of novel phenoxy-N-phenylaniline derivatives were designed and synthesized. The cytotoxicity activities of all the derivatives were measured by MTT assay in different colon cancer cells, 4-(3,5-dimethoxy-4-(((4-methoxyphenethyl)amino)methyl)phenoxy)-N-phenylaniline (42) was discovered, the lead compound 42 with excellent cytotoxicity activity of IC50 = 0.32 μM, IC50 = 0.51 μM, in HT29 and HCT 15 cells, respectively. Compound 42 had a good inhibitory activity of c-Myc/MAX dimerization and DNA binding. Besides, compound 42 could effectively induce apoptosis and induced G2/M arrest in low concentration and G0/G1 arrest in high concentration to prevent the proliferation and differentiation in colon cancer cells. Western blot analysis confirmed the 42 strongly down-regulated expression of c-Myc. Furthermore, during 30 days treatment 42 exhibited excellent efficacy in HT29 tumor xenograft model without causing significant weight loss and toxicity. Consequently, 42 could be a promising drug candidate for CRC therapy.
Phenoxy-N-phenylaniline derivative and application thereof
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Paragraph 0064; 0067; 0069; 0071, (2020/06/05)
The invention relates to a phenoxy-N-phenylaniline derivative and an application thereof, and belongs to the technical field of novel colorectal cancer drugs. The present invention addresses the problem of providing some novel compounds having c-Myc inhibitory activity. The structural formula of the compound is shown as a formula I in the specification. According to the invention, a series of novel phenoxy-N-phenylaniline derivatives are designed and synthesized, and the compounds can be used as c-Myc inhibitors, have a good inhibition effect on the proliferation of colorectal cancer cells, and provide a new choice for colorectal cancer drugs.
A meta-substituted phenol compounds and its preparation method and application
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Paragraph 0051-0055, (2019/05/21)
The invention relates to the field of organic synthesis, in particular relates to a meta-substituted phenol derivative molecule and its preparation method and application. The invention discloses a meta-substituted phenol molecule preparation method, including formula I compounds of the formula II with a compound represented by a plurality of times of oxidative dehydrogenation coupling reaction, a compound represented by formula III. The invention provides a meta-substituted phenol derivative molecule and its preparation method and application, solves the technical intermediate substituted phenol derivatives molecular synthesis reaction and the cost is high, the reaction stability is not high, and the reaction of complex technical issues.
