149353-75-3Relevant articles and documents
Chimeric compound for targeted degradation of androgen receptor protein, preparation method of chimeric compound and application of chimeric compound in medicine
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, (2022/04/03)
The invention relates to a chimera compound for targeted degradation of androgen receptor protein, a preparation method of the chimera compound and application of the chimera compound in medicine. Specifically, the invention relates to a chimera (PROTAC) compound for targeted degradation of AR protein of a fused heterocyclic cerebellar protein (cerebellone) E3 ubiquitin ligase ligand as shown in a general formula (IM), a preparation method of the chimera compound, and application of the chimera compound in medicine, and particularly relates to a chimera (PROTAC) compound for targeted degradation of AR protein of a fused heterocyclic cerebellar protein E3 ubiquitin ligase ligand of a fused heterocyclic cerebellar protein E3 ubiquitin ligase ligand.
Design, synthesis and biological evaluation of a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives as potent fibroblast growth factor receptor (FGFR) inhibitors
Wei, Manman,Peng, Xia,Xing, Li,Dai, Yang,Huang, Ruimin,Geng, Meiyu,Zhang, Ao,Ai, Jing,Song, Zilan
, p. 9 - 28 (2018/05/28)
Starting from the phase II clinical FGFR inhibitor lucitanib (2), we conducted a medicinal chemistry approach by opening the central quinoline skeleton coupled with a scaffold hopping process thus leading to a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives. Compound 25a was identified to show selective and equally high potency against FGFR1/2 and VEGFR2 with IC50 values less than 5.0 nM. Significant antiproliferative effects on both FGFR1/2 and VEGFR2 aberrant cancer cells were observed. In the SNU-16 xenograft model, compound 25a showed tumor growth inhibition rates of 25.0% and 81.0% at doses of 10 mg/kg and 50 mg/kg, respectively, with 5% and 10%body weight loss. In view of the synergistic potential of FGFs and VEGFs in tumor angiogenesis observed in preclinical studies, the FGFR/VEGFR2 dual inhibitor 25a may achieve better clinical benefits.
BENZAMIDE DERIVATIVE USEFUL AS FASN INHIBITORS FOR THE TREATMENT OF CANCER
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, (2015/06/18)
The present invention is directed to benzamide derivatives, pharmaceutical compositions containing them, and their use as FASN inhibitors, in for example, the treatment of cancer, obesity related disorders, liver related disorders and viral infections. Such compounds are represented by formula (I) as follows: wherein R1, R2, R3, R4, R5, m, n, (II) and (III) are defined herein.