Tankyrase inhibitor
A technology of compounds and solvates, applied in the field of tankyrase inhibitors
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preparation example Construction
[0091] The preparation of step 1 intermediate 1
[0092] Dissolve raw material 1 and a basic solvent (such as triethylamine) in an organic solvent (such as dichloromethane), lower the temperature (such as -25 to -10°C), add raw material 2, and keep the reaction at low temperature. After the reaction is complete, concentrate to obtain the intermediate 1.
[0093] Step 2 Preparation of intermediate 2
[0094] Intermediate 2 was purchased or prepared by yourself.
[0095] Step 3 Preparation of Intermediate 3
[0096] Dissolve intermediate 1 in a suitable solvent (such as acetonitrile), add intermediate 2 and a basic substance (such as potassium carbonate), react at 60-90°C (for example, 10-20 hours), complete the reaction, concentrate, and purify (such as Silica gel column chromatography) to obtain intermediate 3.
[0097] Step 4 Preparation of Intermediate 4
[0098] Dissolve intermediate 3 in a suitable solvent (such as dichloromethane), add an acid (such as trifluoroaceti...
experiment example 1
[0134] Experimental Example 1 The in vitro enzymatic activity test of the compound of the present invention
[0135] Test product: the compound of the present invention, its chemical name and preparation method are shown in the preparation examples of the compound.
[0136] (1) Preparation of the test product
[0137] Preparation of the 10mM stock solution of the test product: 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.
[0138] 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 make a series of solutions of concentrations, and then diluted 10 times with water to make solutions containing 10% DMSO, the concentrations were: 100 μM, 10 μM, 1 μM, 0.1 μM.
[0139]
[0140] (2) Experimental...
experiment example 2
[0160] Experimental example 2 The effect of the compound of the present invention on the protein of AXIN2 in SW480 cells
[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) Preparation of the test product
[0163] Weigh 2.00 mg of compound 1, add an appropriate amount of DMSO to dissolve, and mix well to obtain a 10 mM stock solution of compound 1.
[0164] 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.
[0165] (2) Experimental method:
[0166] 1. Cell culture: human colorectal cancer cells SW480, using Leibovitz's L-15 medium + 10% FBS + 1% P...
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