2217-26-7Relevant articles and documents
Synthesis and evaluation of highly selective quinazoline-2,4-dione ligands for sphingosine-1-phosphate receptor 2
Gropler, Robert J.,Klein, Robyn S.,Liu, Hui,Luo, Zonghua,Tu, Zhude,Yu, Yanbo
, p. 202 - 207 (2022/03/30)
A series of twenty-nine new quinazoline-2,4-dione compounds were synthesized and their IC50 values for binding toward sphingosine-1-phosphate receptor 2 (S1PR2) were determined using a [32P]S1P binding assay. Seven compounds 2a, 2g, 2h, 2i, 2j, 2k, and 5h exhibit high S1PR2 binding potencies (IC50 values 98%), and high molar activity (153-222 GBq μmol-1, at the end of bombardment). [11C]2a and [11C]2i were further evaluated by the ex vivo biodistribution study. The results showed that both tracers have low brain uptake, preventing their potential for neuroimaging application. Further explorations of this class of S1PR2 PET tracers in peripheral tissue diseases are underway. This journal is
2,4-DIOXO-QUINAZOLINE-6-SULFONAMIDE DERIVATIVES AS INHIBITORS OF PARG
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Paragraph 00199; 00200, (2016/07/05)
The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity wherein R1a, R1b, R1c, R1d, R1e, W, X1, X2, X3, X4, X5, X6, X7, c are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which PARG activity is implicated.
Molybdenum-mediated synthesis of quinazolin-4(3H)-ones via cyclocarbonylation using microwave irradiation
Roberts, Bryan,Liptrot, David,Luker, Tim,Stocks, Michael J.,Barber, Catherine,Webb, Nicola,Dods, Robert,Martin, Barrie
supporting information; experimental part, p. 3793 - 3796 (2011/08/06)
A new, efficient and practical synthesis of quinazolin-4(3H)-ones is reported via molybdenum-mediated cyclocarbonylation using microwave irradiation. These methods allow access to a wide range of quinazolin-4(3H)-ones in reasonable yields without the need for gaseous carbon monoxide and palladium catalysts. A range of reactions illustrating the wide scope of this chemistry was carried out and all proceeded in reasonable yields.