54901-09-6Relevant academic research and scientific papers
Pyrazole derivative for FGFR inhibitor and preparation method of pyrazole derivative
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Paragraph 0214-0216, (2021/03/06)
The invention provides a pyrazole derivative for an FGFR inhibitor and a preparation method of the pyrazole derivative. The invention specifically relates to an amide pyrazole compound serving as an FGFR irreversible inhibitor, and a preparation method and application thereof. The present invention provides a compound as shown in Formula I, or a pharmaceutically acceptable salt, or solvate, isotope substitute, prodrug, or metabolite thereof. The compound as shown in general formula I have FGFR inhibitory activity, and is capable of preventing or treating disorders associated with FGFR activityor expression, preferably such as cancer.
Vinyl sulfamido substituted pyrazolyl benzamide compound
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Paragraph 0093-0094, (2020/07/02)
The invention provides a vinyl sulfamide substituted pyrazolyl benzamide compound. Specifically, the present invention provides a compound in formula I shown in the specification or a pharmaceuticallyacceptable salt thereof, and a preparation method and use thereof. The compound shown in the formula I has excellent FGFR inhibitory activity and can be used for preventing or treating diseases related to FGFR kinase activity or expression quantity, such as cancer.
Asymmetric total synthesis of dihydroisocoumarins: 6-methoxymellein, kigelin and fusarentin 6, 7 dimethyl ether by employing proline catalysed asymmetric α-aminoxylation
Mane, Baliram B.,Markad, Sachin B.,Waghmode, Suresh B.
, (2020/10/19)
A concise asymmetric total synthesis of dihydroisocoumarins such as 6-methoxymellein, kigelin and fusarentin 6,7-dimethyl ether in high enantiopurity have been achieved from non-chiral aldehydes by employing proline catalysed asymmetric α-aminoxylation reaction. The required stereochemistry of hydroxyl group have been generated by alternating L or D proline as a organocatalyst in α-aminoxylation step and lactone ring is assembled by oxa-Pictet-Spengler cyclisation reaction as the key steps.
Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors
Fan, Jun,Dai, Yang,Shao, Jingwei,Peng, Xia,Wang, Chen,Cao, Sufen,Zhao, Bin,Ai, Jing,Geng, Meiyu,Duan, Wenhu
supporting information, p. 2594 - 2599 (2016/05/09)
Fibroblast growth factor receptors (FGFRs) are important oncology targets due to the dysregulation of this signaling pathway in a wide variety of human cancers. We identified a series of pyrazolylaminoquinazoline derivatives as potent FGFR inhibitors with low nanomolar potency. The representative compound 29 strongly inhibited FGFR1-3 kinase activity and suppressed FGFR signaling transduction in FGFR-addicted cancer cells; FGFRs-driven cell proliferation was also strongly inhibited regardless of mechanistic complexity implicated in FGFR activation, which further confirmed that 29 was a potent pan-FGFR inhibitor. The flexibility of our structure offered the potential to preserve good affinity for mutant FGFR, which is important for developing TKIs with long-term efficacy.
A convenient and effective synthesis of 3-(3,5-dimethoxyphenyl)propanal
Nikas, Spyros P.,Thakur, Ganesh A.,Makriyannis, Alexandros
, p. 1751 - 1756 (2007/10/03)
A convenient and effective synthesis of 3-(3,5-dimethoxyphenyl) propanal, an important intermediate in the synthesis of various biologically active compounds is described.
