17481-62-8Relevant academic research and scientific papers
Structure-activity relationship of spop inhibitors against kidney cancer
Dong, Ze,Wang, Zhen,Guo, Zhong-Qiang,Gong, Shouzhe,Zhang, Tao,Liu, Jiang,Luo, Cheng,Jiang, Hualiang,Yang, Cai-Guang
, p. 4849 - 4866 (2020/06/08)
Speckle-type POZ protein (SPOP) is overexpressed in the nucleus and misallocated in the cytoplasm in almost all the clear-cell renal cell carcinomas (ccRCCs), which leads to kidney tumorigenesis. Previously, we elucidated that the oncogenic SPOP-signaling pathway in ccRCC could be suppressed by 6b that inhibits SPOP-mediated protein interactions. Herein, we have established a structure-activity relationship for 6b analogues as SPOP inhibitors. Compound 6lc suppresses the viability and inhibits the colony formation of ccRCC cell lines driven by cytoplasmic SPOP, superior to 6b. Compound 6lc binds to the SPOP protein in vitro and disrupts SPOP binding to phosphatase-and-tensin homologue (PTEN) in HEK293T cells, which causes the observable phenomena: a decline in the ubiquitination of PTEN, elevated levels of both PTEN and dual-specificity phosphatase 7, and decreased levels of phosphorylated AKT and ERK when ccRCC cell lines are exposed to 6lc in a dose-response manner. Taken together, compound 6lc is a potent candidate against kidney tumorigenesis.
Characterization and structure-activity relationship study of iminodipyridinopyrimidines as novel hepatitis C virus inhibitor
Park, Dong-Sik,Jo, Eunji,Choi, Jihyun,Lee, MyungEun,Kim, Soohyun,Kim, Hee-Young,Nam, Jiyon,Ahn, Sujin,Hwang, Jong Yeon,Windisch, Marc Peter
, p. 65 - 73 (2017/09/20)
Upon high-throughput screening of synthetic small molecule libraries with the infectious hepatitis C virus (HCV) cell culture system, we identified an iminodipyridinopyrimidine (IDPP) scaffold. IDPP did not inhibit HCV replication, but exhibited very potent inhibitory activity on early and late steps of HCV life cycle. Applying an intensive structure-activity relationship (SAR) study, a promising IDPP Lead compound (12c) with excellent potency (EC50 = 10 nM), high safety margin (SI > 2000), and an acceptable stability in human and rat liver microsomes (t1/2 >60 min) was identified. Overall, our results suggest that the IDPP scaffold could be used for the development of novel HCV interventions.
NOVEL MEDICINAL COMPOUNDS
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Page/Page column 27-28, (2011/08/08)
The present invention concerns novel compounds possessing the general formula (I), pharmaceutical preparations containing such active ingredients, as well as the process for manufacture thereof, where R, X, A and Q are defined in the claims. The novel compounds are efficient in the prevention and/or treatment of diseases caused by the bacterium Mycobacterium tuberculosis or any other Mycobacteria.
