134179-40-1Relevant articles and documents
Synthesis of copolymers alternating oligophenylenevinylene subunits and fullerene moieties
Gutiérrez-Nava, Manuel,Masson, Patrick,Nierengarten, Jean-Fran?ois
, p. 4487 - 4490 (2003)
Linear polymers alternating oligophenylenevinylene (OPV) moieties and C60 subunits have been prepared in good yields by polycondensation of a bifunctional fullerene derivative with an OPV monomer bearing two alcohol functions. These polymers ha
Targeted selective degradation of Bruton’s tyrosine kinase by PROTACs
Da, Yang,Lin, Jun,Lin, Pei,Liu, Shaodong,Shu, Yongzhi,Wang, Feng,Yan, Renjie
, (2020)
Bruton’s tyrosine kinase (BTK) is critical for B-cell receptor signaling and related to many types of human cancers. However, the drug resistance and off-target effect of present traditional BTK inhibitors occurred over time. As a new strategy for drug development, the proteolysis targeting chimera (PROTAC) has been proved to target varieties of proteins. Here SPB5208 (4-(2-(2-(2-(2-(3-(4-amino-3-(4-phenoxy phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)ethoxy)ethoxy)ethoxy)ethoxy)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione) was synthesized as a new PROTAC degradation agent of BTK by linking Ibrutinib and Thalidomide. In vitro study indicated that SPB5208 reduced the BTK enzyme activity with high selectivity and inhibited effectively cancer cell proliferation. More than that, SPB5208 induced BTK protein degradation through a proteasome- and CRBN- dependent manner in JeKo-1 cells. In addition, SPB5208 was also confirmed to induce significantly BTK protein degradation in vivo. Thus, this study provides a new pharmacological tool for further study of new BTK PROTAC and their mechanism of action in physiological environment.
Prodrug compound and application ofprodrug compound in treatment of cancer
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Paragraph 0204-0205, (2021/03/06)
The present invention provides a compound indicated by a formula (I), pharmaceutically acceptable salts or esters thereof, a pharmaceutical composition of the compound, and application of the compoundand the pharmaceutical composition in the inhibition or regulation of the activity of tyrosine kinase and treating disease symptoms or symptoms including cancer mediated by tyrosine kinase.
DEFINED MONOMER SEQUENCE POLYMERS
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Paragraph 0075; 0117-0119, (2018/09/21)
Processes of preparing defined monomer sequence polymers are disclosed, in which a backbone portion of the polymer is first prepared by performing one or more sequential monomeric coupling reactions with intervening membrane diafiltration purification/isolation steps, followed by a step of decorating the backbone portion with one or more side chains at predetermined positions along its length. The process represents an improvement on prior art techniques, which impose limitations on the size of the side chains that may be present. Defined monomer sequence polymers that are obtainable by the processes are also disclosed.
