98262-66-9Relevant articles and documents
PYRROLIDINYL UREA DERIVATIVES AND APPLICATION THEREOF IN TRKA-RELATED DISEASES
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Paragraph 0153; 0154; 0155, (2021/05/21)
The present invention relates to a class of TrkA inhibitors and an application thereof in the preparation of a drug for the treatment of diseases associated with TrkA. The present invention specifically discloses compounds represented by formula (I) and f
MACROCYCLIC INDOLES AS MCL-1 INHIBITORS
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Paragraph 1286-1287, (2020/06/10)
Disclosed is compound of formula I and the pharmaceutically acceptable salts and solvates thereof, wherein R, R1a, R1b, R1h, L1, L2, L3, ?, ?, ? are as defined as set forth in the specification. Disclosed is compound of formula I for use to treat a condition or disorder responsive to Mcl-1 inhibition such as cancer.
Design, synthesis and biological evaluation of ring-fused pyrazoloamino pyridine/pyrimidine derivatives as potential FAK inhibitors
Xie, Hongming,Lin, Xinglong,Zhang, Yingjun,Tan, Fuxing,Chi, Bo,Peng, Zhihong,Dong, Wanrong,An, Delie
supporting information, (2020/10/06)
We report herein the synthesis of novel ring-fused pyrazoloamino pyridine/pyrimidine derivatives as potential FAK inhibitors and the evaluation of pharmaceutical activity against five cancer cell lines (MDA-MB-231, BXPC-3, NCI-H1975, DU145 and 786O). Generally, the majority of compounds displayed strong anti-FAK enzymatic potencies (IC50 1 nM) and could effectively inhibit several class of cancer cell lines within the concentration of 3 μM in comparison with GSK2256098 as a reference. Among them, compound 4o is considered to be the most effective due to high sensitivity in antiproliferation. In culture, 4o could not only inhibit FAK Y397 phosphorylation in MDA-MB-231 cell line, but also trigger apoptosis in a dose-dependent manner. Furthermore, computational docking analysis also suggested that 4o and TAE-226 displayed the similar interaction with FAK kinase domain.