Anti-metastatic effects of 2,4,7-trisubstituted pyrimidoindole compounds
A compound and composition technology, applied in 2 fields, can solve problems such as family and social influence
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[0030] In one aspect, the present invention provides the compound 2-benzyl-4-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline-2-ethylamino)-7-(2- Methyltetrazol-5-yl)pyrimidin[4,5]indole, or an isomer, prodrug, pharmaceutically acceptable salt or solvate thereof.
[0031] Its structure is shown in the following formula:
[0032]
[0033] In one aspect, the invention provides a compound selected from any subset list of compounds within the scope of the exemplary embodiments, or an isomer, prodrug, pharmaceutically acceptable salt or solvate thereof.
[0034] III. Other embodiments of the present invention
[0035] In another embodiment, the present invention provides a pharmaceutical composition comprising at least one compound of the present invention or a process for the preparation of an isomer, prodrug, pharmaceutically acceptable salt or solvate thereof, Include the following steps:
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Embodiment 1
[0062]Example 1: 2-benzyl-4-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline-2-ethylamino)-7-(2-methyl tetrazo Synthesis of Azol-5-yl)pyrimidin[4,5]indole (XH003)
[0063] 1.1 Synthesis of 5-(3-nitrophenyl)tetrazolium (B001)
[0064]
[0065] Take 30.0g (202.69mmol) of m-nitrobenzonitrile, 14.5g (222.96mmol) of sodium azide, and 45.7g (202.69mol) of zinc bromide in a 1000ml flask, add 500ml of water, reflux at 100°C for 24h, then cool down To room temperature, pour the reaction solution into 500ml of water, add 100ml of 3N hydrochloric acid, extract with ethyl acetate (3×200ml), collect the organic phase, spin dry the ethyl acetate under reduced pressure to obtain a white solid, add 800ml of 0.25mol / L NaOH, stirred, the solid dissolved first and then re-precipitated white flocculent zinc hydroxide, suction filtered, the filtrate was adjusted to pH=5 with 3.0mol / L hydrochloric acid, a large amount of white solid was precipitated, and the dry white product was 34.8g, the yield ...
Embodiment 2
[0099] Example 2: Effect of Compound XH003 on Migration Experiment of Breast Cancer MCF-7 Cells
[0100] Take MCF-7 cells in the logarithmic growth phase, wash away dead cells and dead cell debris with PBS, digest with 0.25% trypsin and blow into single cells, trypsinize and centrifuge, use serum-free DMEM medium to adjust cell density 2.5×10 5 cells / ml, 100 μl of the counted cell suspension was added to the Transwell chamber for culture, and then XH003 (1 μM, 2.5 μM, 5 μM), 5 μM cisplatin (positive control group), and complete medium (blank control group) were added respectively. Add 500 μl complete medium containing 10% FBS to the lower chamber of the 24-well plate. After 48 hours, take out the small chamber and suck up the medium, wash the small chamber twice with PBS, fix in 4% paraformaldehyde for 30 minutes, stain with 0.1% crystal violet for 20 minutes, wipe off Matrigel and cells in the upper chamber with a cotton swab, and wash three times with PBS , using an invert...
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