26268-04-2Relevant articles and documents
High-affinity CD169 anti-tumor compound, and preparation method and application thereof
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Paragraph 0065; 0066; 0067; 0068; 0069; 0070; 0071-0076, (2018/03/24)
The invention provides a high-affinity CD169 anti-tumor compound, and a preparation method and application thereof. The high-affinity CD169 anti-tumor compound is a small-molecular anti-tumor compound that can kill tumors with its specific and broad-spectrum properties. TCC-Neu5Ac is targeted an in-vivo tumor and metabolically grows on the surfaces of tumor cells to form TCC-Neu5Ac ligand; macrophages near the tumor recognize and phagocytose the TCC-Neu5Ac ligand, releases tumor fragments and presents the tumor fragments to other immune cells so as to trigger anti-tumor immune responses. The high-affinity CD169 anti-tumor compound provided by the invention is effective to a variety of tumors and also has inhibitory effect on tumor metastasis. In addition, the high-affinity CD169 anti-tumor compound provided by the invention not only can be injected but also can be orally taken, and has extremely low cytotoxicity and animal toxicity, broad application prospects and good market value.
Synthesis and Biological Activity of 4H-Thieno[3,2-c]Chromene Derivatives
Bogza, Yu. P.,Katsiel',Sharypova,Tolstikova,Fisyuk
, p. 1712 - 1718 (2015/02/05)
The formyl group of 4H-thieno[3,2-c]chromene-2-carbaldehyde was transformed into the respective nitrile, amide, ester, carboxylic, hydroxamic, or hydroxy group. Electrophilic substitution in 4H-thieno[3,2-c]chromene-2-carbaldehyde was shown to occur at the C-8 atom, while oxidation with 2,3-dichloro-5,6-dicyano-1,4-benzoquinone in methanol led to 4-methoxy-4H-thieno[3,2-c]chromene-2-carbaldehyde. The latter compound was found to possess high antiulcer activity.
Structure-based design of thienobenzoxepin inhibitors of PI3-kinase
Staben, Steven T.,Siu, Michael,Goldsmith, Richard,Olivero, Alan G.,Do, Steven,Burdick, Daniel J.,Heffron, Timothy P.,Dotson, Jenna,Sutherlin, Daniel P.,Zhu, Bing-Yan,Tsui, Vickie,Le, Hoa,Lee, Leslie,Lesnick, John,Lewis, Cristina,Murray, Jeremy M.,Nonomiya, Jim,Pang, Jodie,Prior, Wei Wei,Salphati, Laurent,Rouge, Lionel,Sampath, Deepak,Sideris, Steve,Wiesmann, Christian,Wu, Ping
scheme or table, p. 4054 - 4058 (2011/08/06)
Starting from thienobenzopyran HTS hit 1, co-crystallization, molecular modeling and metabolic analysis were used to design potent and metabolically stable inhibitors of PI3-kinase. Compound 15 demonstrated PI3K pathway suppression in a mouse MCF7 xenogra