Tankyrase inhibitor
A technology of compounds and solvates, applied in the field of tankyrase inhibitors
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preparation example Construction
[0106] Step 1 Preparation of intermediate 1
[0107] Intermediate 1 was obtained by purchase or preparation.
[0108] Step 2 Preparation of Intermediate 2
[0109] Intermediate 1 and raw material 1 were dissolved in an appropriate solvent (such as a mixed solution of triethylamine and N,N-dimethylformamide), and the reaction was complete at room temperature. Water and an organic solvent (such as dichloromethane) were added to separate the layers. The organic phase is dried, concentrated, and purified (eg, silica gel column chromatography) to obtain intermediate 2.
[0110] Step 3 Preparation of Intermediate 3
[0111] Dissolve intermediate 2 in a suitable solvent (such as tetrahydrofuran), add raw material 2 at 0°C, react at room temperature (for example, 10-20 hours), complete the reaction, filter, add water and an organic solvent (such as dichloromethane), and separate the layers , the organic phase was dried, concentrated, and purified (eg, silica gel column chromatograp...
experiment example 1
[0160] Experimental example 1 In vitro enzymatic activity test of the compound of the present invention
[0161] Test product: the compound of the present invention, its chemical name and preparation method are shown in the preparation examples of the compound.
[0162] (1) Compound preparation
[0163] Preparation of compound 10mM stock solution: Weigh an appropriate amount of the test product (see the table below for the specific weighing amount), add an appropriate amount of DMSO to dissolve, mix well, and set aside.
[0164] 10 mM stock solution was taken respectively, and diluted with DMSO to a solution with a concentration of 1 mM, which was used as the mother solution. The above mother solution was diluted 10 times with DMSO to prepare a series of solutions with concentrations, and then diluted 10 times with water to prepare solutions containing 10% DMSO, the concentrations were: 100 μM, 10 μM, 1 μM, 0.1 μM.
[0165]
[0166] (2) Experimental method
[0167] 1. Pre...
experiment example 2
[0193] Experimental example 2 The effect of the compound of the present invention on the protein of AXIN2 in SW480 cells
[0194] Test product: the compound of the present invention, its chemical name and preparation method are shown in the preparation examples of the compound.
[0195] (1) Preparation of the test product
[0196] Preparation of compound 10mM stock solution: Weigh an appropriate amount of compound (see the table below for the specific weighing amount), add appropriate amount of DMSO to dissolve, mix well, and set aside.
[0197] Take 10mM stock solutions respectively, and dilute the above mother solutions step by step with DMSO to make mother solutions with concentrations of 1mM and 0.2mM (×1000), then dilute them 1000 times with culture medium, and then add them to the corresponding wells of the 6-well plate. The final concentration of the obtained compound solution was: 1 μM, 0.2 μM.
[0198]
[0199] (2) Experimental method
[0200] 1. Cell culture:...
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