Improved treatment of renal cell carcinoma
A renal cell carcinoma, cytotoxic technology, applied in the field of cancer treatment, can solve problems such as tissue damage, achieve the effect of improving quality of life, reducing stress, and avoiding dialysis treatment
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Embodiment 1
[0112] Synthesis of Orellanine
[0113] Orellanine was synthesized from commercially available 3-hydroxypyridine essentially as described by others. (Tiecco M, Tingoli M, Testaferri L, Chianelli D and Wenkert E: Total synthesis of Orellanine, the lethal toxin of Cortinarius orellanus Fries Mushroom. Tetrahedron 42, 1475-1485(1986).
Embodiment 2
[0115] Orellanine conjugated to polyethylene glycol (PEG)
[0116] A. Conjugate on carbon
[0117] A solution of lithium diisopropylamide (LDA) was prepared at -23°C from diisopropylamine (0.77ml, 5.50mmol) and 1.55M n-butyllithium (3.55ml, 5.50mmol) in 10ml tetrahydrofuran (THF). After 15 minutes, 3,3',4,4'-tetramethoxy-2,2'-bipyridine-bis-N-oxide (1.54 g, 5.00 mmol) was added and the resulting mixture was stirred at -23°C 30 minutes. 1-Bromo-2-(2-methoxyethoxy)ethane (1.19 g, 6.50 mmol) was added and the reaction mixture was stirred at -23°C for 15 minutes and at room temperature for 1 hour. Water (10ml) and diethyl ether (10ml) were added and the layers were separated. The aqueous phase was extracted with diethyl ether (3 x 25ml). The combined organic extracts were washed with 25ml portions of water and brine. in anhydrous Na 2 SO 4 After drying, the solvent was removed in vacuo to give the crude product. By flash chromatography (SiO 2 , 25% EtOAc in hexanes) aff...
Embodiment 3
[0125] Label Orellanine with Astatine 211 (At-211)
[0126] 13 mg, 0.051 mmol Orellanine and 32.8 mg of 0.3 mmol sodium carbonate were dissolved in 1.2 ml of water. lodoGen beads (Thermo Fisher Scientific, Rockford, IL) were added followed by 0.20 mmol of radioactive iodine in the form of NaI. The mixture was stirred at room temperature for 90 minutes. The mixture was then filtered to remove the lodoGen beads, and the filtrate was washed with 42 mg NaHSO 4 acidification. Labeled Orellanine was isolated by preparative HPLC.
[0127] Similarly, preparations produced by irradiating native Bi with 28 MeV α particles, with 211 At radiohalogenated orellanine derivatives, purified by distillation, collected in Teflon tubes. Except for Orellanine synthesized according to Example 1, all standard chemicals were purchased from local merchants.
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