89567-04-4Relevant articles and documents
For FGFR1 tetrahydroben-and thieno [2, 3 - d] amino pyrimidine derivative and its preparation method and application
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, (2018/02/22)
The invention relates to tetrahydrobenzothieno[2,3-d]aminopyrimidine derivatives acting on FGFR1, and a preparation method and application thereof. The structure of the tetrahydrobenzothieno[2,3-d]aminopyrimidine derivatives is disclosed as Formula (I). The anti-apoptosis experiment research on the three cells H460 (human lung cancer cell), A549 (human lung adenocarcinoma cell) and U251 (glioma cell) indicates that all the detected compounds have certain inhibition activity, and the inhibition activity increases as the concentration increases. Meanwhile, the FGFR1 kinase inhibition activity experiment indicates that the compounds have certain antitumor activity.
New insight into adenosine receptors selectivity derived from a novel series of [5-substituted-4-phenyl-1,3-thiazol-2-yl] benzamides and furamides
Inamdar, Gajanan S.,Pandya, Amit N.,Thakar, Hardik M.,Sudarsanam, Vasudevan,Kachler, Sonja,Sabbadin, Davide,Moro, Stefano,Klotz, Karl-Norbert,Vasu, Kamala K.
, p. 924 - 934 (2013/07/27)
A series of [5-substituted-4-phenyl-1,3-thiazol-2-yl] benzamide and furamide analogues were investigated in radioligand binding studies at adenosine receptor subtypes with an aim to obtain potent and selective adenosine receptor ligands. Benzamide and furamide linked to thiazole was found to be crucial for high adenosine receptor affinity. The most potent compound indentified in this study was 5d with low nanomolar affinity for all four adenosine receptor subtypes. Compounds 5a and 5g showed moderate selectivity for A2A adenosine receptors. Molecular docking versus all four human adenosine receptors combined with membrane molecular dynamics studies were performed to rationalise the peculiar selectivity profile of 5d antagonist.