Novel metalloporphyrins and their uses as radiosensitizers for radiation therapy
A radiosensitizer and compound technology, applied in the field of brain tumors and head and neck tumors, can solve problems such as ineffectiveness
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Embodiment 1
[0061] In this example, CuTCPBr was synthesized from CuTCPH by the bromination method. CuTCPH (200 mg, 0.146 mmol) was dissolved in a 1:1 mixed solvent of chloroform and carbon tetrachloride (70 mL). While stirring the mixture, bromine (240 μL, 4.6 mmol) dissolved in the same mixed solvent (20 mL) was added over 30 minutes. Pyridine (0.6 mL) dissolved in a mixed solvent (15 mL) was added over 30 minutes, followed by stirring at room temperature overnight. Excess bromine was removed the next day with 20% aqueous sodium metabisulfite (40 mL). The reaction mixture was worked up, and the organic layer was separated and washed 3 times with water. The organic layer was then dried over anhydrous sodium sulfate, and the solvent was removed in vacuo. The desired product was purified by preparative thin layer chromatography. The product weighs 176 mg (0.088 mmol), and the yield is 60%.
[0062] Compounds were identified by optical absorption spectroscopy and fast atom bombardment m...
Embodiment 2
[0064] Thoracic and back tumors
[0065] Five BALB / c mice implanted subcutaneously with EMT-6 breast cancer in the chest and back were injected intraperitoneally (ip) six times with a total dose of CuTCPBr of 186 μg / g body weight in 2 days. Four days after the last injection, the mice were euthanized and the mean boron concentration (μg / g wet tissue) of the different tissues was determined. The results are shown in Table 1.
[0066] sample
[0067] No somatic or behavioral toxic effects on mice were observed during and after porphyrin administration. Necropsy revealed that all tissues were normal.
Embodiment 3
[0069] leg tumor
[0070] In this example, BALB / c mice with subcutaneous EMT-6 leg tumors were administered 156 μg CuTCPBr / g body weight within 2 days, with a volume of 0.01 mL / g body weight / injection. Next, the boron concentration (μg / g) in various tissues of BALB / c mice was measured, and the results are shown in Table 2.
[0071] last note
days since ejaculation
number of mice
the tumor
Blood
the brain
Ear
liver
2
6
24±11
0.2±0.1
0±0.1
1±1
271±40
5
5
13±6
0.1±0.1
0.6±1
0.6±0.7
308±40
[0072] Notably, boron concentrations in leg tumors were significantly lower than those in thoracic and back tumors. There is larger vasculature around the thorax and back compared to the legs, which may be a factor. However, when it was CuTCPH, the boron concentration in the leg tumors was 30% highe...
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