Application of substituted 5,6-dihydroisoquinoline [3,2-alpha]isoquinoline-7-onium derivative
A technology of dihydroisoquinoline and isoquinoline, which can be applied to medical preparations containing active ingredients, drug combinations, organic active ingredients, etc. The effect of high selectivity and good application prospects
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Embodiment 1
[0039] This embodiment discloses biopharmaceutical acceptable compounds, salts, and crystal forms with substituted 5,6-dihydroisoquinolino[3,2-α]isoquinolin-7-onium derivatives as the main active ingredient , The use of solvates to prepare inhibitors, the inhibitors can be used directly or in the form of pharmaceutical compositions, and the inhibitory targets are METL3 and METL14.
[0040] The structure of the substituted 5,6-dihydroisoquinolino[3,2-α]isoquinolin-7-onium derivative is shown in formula I:
[0041]
[0042] Where R 1 As -H, -CF 3 , -NO 2 , -OCF 3 , Benzyl, C 1 ~C 8 Alkoxy, C 3 ~C 8 Cycloalkyl, halogen or substituted 5- to 12-membered unsaturated heterocyclic ring; when substituted 5- to 12-membered unsaturated heterocyclic ring, the unsaturated heterocyclic ring contains 1 to 4 heteroatoms, and the heteroatoms are N, O or S;
[0043] R 2 As -H, -CF 3 , -NO 2 , -OCF 3 , Benzyl, C 1 ~C 8 Alkoxy, C 3 ~C 8 Cycloalkyl, halogen or substituted 5- to 12-membered unsaturated h...
Embodiment 2
[0047] This example discloses several compounds based on the compound formula I in the above examples, and the structures are as follows:
[0048]
Embodiment 3
[0050] This embodiment discloses the differential fluorescence scanning test experiment of the seven compounds in the above embodiment, the purpose of which is to detect the stability of the compound to the three-dimensional structure of methyltransferase in vitro. In this experiment, the differential fluorescence scanning (Differential Scanning Fluorimetry) test method was used to test the stability of METL3 in vitro. The stability of the test compound can be expressed by Tm (protein denaturation temperature difference).
[0051] 1. Experimental materials
[0052] Human METTL3, SYPRO orange dye (Sigma, 5000X concentrate in DMSO, S5692), RT-PCR detection system (BIO-RAD CFX96), buffer (20mM Hepes, PH 7.4, and 100mM NaCl).
[0053] All 5,6-dihydroisoquinolino[3,2-α]isoquinoline-7-onium derivatives tested were purchased from Target Molecule (USA).
[0054] For in vitro experiments, it was prepared with 100% DMSO to prepare a 10mM storage solution, stored in a refrigerator at -20°C and ...
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Abstract
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