87394-48-7Relevant articles and documents
PYRIMIDO[5,4-d]PYRIMIDINE DERIVATIVES AS ENT INHIBITORS FOR THE TREATMENT OF CANCERS, AND COMBINATION THEREOF WITH ADENOSINE RECEPTOR ANTAGONISTS
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Page/Page column 134; 173, (2021/09/04)
The present invention relates to pyrimido[5,4-d]pyrimidine derivatives of formula (I), including pharmaceutically acceptable salts and solvates thereof. Compounds of the invention are inhibitors of ENT family transporter, especially of ENT1, and are useful as therapeutic compounds for the treatment of cancers. The invention also relates to the combined use of the pyrimido[5,4-d]pyrimidine derivatives with an adenosine receptor antagonist, for the treatment of cancers.
Strategy for 14C-labeling of a series of bis(heteroaryl) piperazines
Arjomandi, Omid Khalili,Saemian, Nader,Shirvani, Gholamhossein,Javaheri, Mohsen,Esmailli, Kameh
scheme or table, p. 363 - 366 (2012/06/04)
Four bis(heteroaryl)piperazines labeled with carbon-14 in the 2-position of imidazole moiety were prepared as part of a 4-step (or 5-step) sequence from 5-hydroxymethyl-2-mercapto-1-benzylimida-zole-[2-14C] as a key synthetic intermediate which
Discovery and Initial SAR of Arylsulfonylpiperazine Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1)
Sun, Daqing,Wang, Zhulun,Di, Yongmei,Jaen, Juan C.,Labelle, Marc,Ma, Ji,Miao, Shichang,Sudom, Athena,Tang, Liang,Tomooka, Craig S.,Tu, Hua,Ursu, Stefania,Walker, Nigel,Yan, Xuelei,Ye, Qiuping,Powers, Jay P.
scheme or table, p. 3513 - 3516 (2009/04/11)
High-throughput screening of a small-molecule compound library resulted in the identification of a series of arylsulfonylpiperazines that are potent and selective inhibitors of human 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1). Optimization of the initial lead resulted in the discovery of compound (R)-45 (11β-HSD1 IC50 = 3 nM).