Tumor imaging compound, its preparation method and application in tumor diagnostic imaging
A compound and contrast agent technology, applied in the field of tumor imaging compounds, can solve the problems of non-specific recognition of tumor tissue, insufficient sensitivity, and short imaging time.
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[0182] IV. Preparation of Formula I Compounds
[0183] The present invention also provides the method for preparing the compound of formula I' of the present invention, comprises the compound shown in following formula 1 and compound Z-R 22 Reaction, thereby obtain the compound shown in formula I ':
[0184]
[0185] In the formula, X - , R 1 -R 8 , n 1 -n 2 , R 21 and R 22 As described in any embodiment of the preceding formula I'; the selection of Y and Z allows the reaction to obtain L of the present invention, i.e. *-T 1 -C(O)-, *-C(O)-T 1 -,*-S(O) 2 -T 2 - and *-T 2 -S(O) 2 -, where T 1 and T 2 As described in any of the preceding embodiments. For example, Y could be -NH 2 , -COOH, -OH, -SH, -C(O)-X', -S(O) 2 -X' or -S(O) 2 OH, Z can be correspondingly a group that can react with Y, such as -NH 2 , -COOH, -OH, -SH, -C(O)-X', -S(O) 2 -X' or -S(O) 2 OH, to form such as -C(O)-NH-, -NH-(CO)-, -C(O)-O-, -O-C(O)-, -S(O) 2 -NH-, -NH-S(O) 2 -, -S(O) 2 -...
Embodiment 1
[0199] Embodiment 1: the preparation of formula II compound
[0200]
[0201] In the formula, T can be selected from O, NH or S; R is the R of the present application 22 .
[0202] The compound of formula II can be prepared by the following steps:
[0203] At low temperature, under the protection of an inert gas, the equivalent of compound 3 and compound 9 were dissolved in methylene chloride and stirred at a low speed, and 1 equivalent of 1-(3-dimethylaminopropyl)-3-ethyl carbon was slowly added dropwise within 2 hours. Diimine hydrochloride and a catalytic amount of 4-dimethylaminopyridine in dichloromethane. The mixture was stirred at low speed for 24 hours. After the completion of the reaction was monitored by silica gel thin-layer chromatography, dichloromethane was added, washed with brine, and dried overnight over anhydrous sodium sulfate. Purified by silica gel column chromatography (methanol / dichloromethane), the final purified product was a green powdery solid....
Embodiment 2
[0234] Example 2: Fluorescence localization imaging of compounds 1-3, 4, 5 and 7 in human renal carcinoma cell line 786o.
[0235] 786o cells (3×10 5 / well) were inoculated in a 6-well plate in advance, placed in a cell culture incubator for 48 h, blotted dry medium, added medium containing the corresponding compound (5 μM) and Mito-tracker (0.2 nM) to the experimental well, incubated for 30 min, Washed with PBS solution 3 times, imaged using a fluorescence microscope equipped with an infrared camera and a continuous LED light source. The near-infrared shooting conditions are Ex=745nm, Em=820nm; the Mito-tracker shooting conditions are Ex=488nm, Em=520nm.
[0236] The experimental results of compounds 1-3, 4, 5 and 7 are as follows Figure 1-6 shown.
[0237] The results show that compounds 1-3, 4, 5 and 7 can be taken up by tumor cells, and their intracellular distribution can basically be co-localized with the distribution of Mito-tracker. Mito-tracker can mark the mitoch...
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