Application of C60-benzoic acid nitrogen mustard in preparing medicine for anti tumor
An antineoplastic drug, the technology of benzoate nitrogen mustard, which is applied in the direction of antineoplastic drugs, drug combinations, pharmaceutical formulations, etc., can solve the problems of nitrogen mustards with high toxicity and side effects, and the application of no reported compounds
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[0014] C 60 -Preparation of Benzoambucil (for details, see document V.P.Gubskaya, N.P.Konovalova et al.Synthesis of new functionally substituted fullereopyrrolidines.Russian Chemical Bulletin, International Edition, Vol.51, No.9, pp.1723-1726)
[0015] 216mg (0.6mmol) C 60 (Fullerene) was dissolved in 200mL toluene, 53mg (0.6mmol) sarcosine and 74mg (0.3mmol) benzaldehyde nitrogen mustard were added, heated to reflux in an oil bath at 110°C for 10h, the solution changed from purple to red. The resulting solution was rotary evaporated to dryness to obtain a brownish black solid, which was separated by column chromatography (silica gel H300-400 mesh, packed with n-hexane). : 1 n-hexane and toluene eluent rinse, wash down C 60 For the mono-adduct, the solvent was evaporated to obtain 96 mg of a tan solid with a yield of 42%.
Embodiment 1
[0016] Example 1 125 I-C 60 -Distribution of Benzoambucil in Rats
[0017] C 60 - Radioactive labeling of benzoen mustard
[0018] a.C 60 - Iodination of benzoen mustard Weigh 11mg C 60 - Benzoambucil dissolved in 30mL CH 2 Cl 2 and 5mL CHCl 3 Add about 2 mL of ICl solution to the mixed solvent, and react at room temperature for 5 days in the dark; use 50 mL of 10% Na 2 S 2 o 3 The excess ICl was washed off twice, the organic phase was concentrated, and a dark brown product band was collected through a silica gel column.
[0019] b. 125 Isotope exchange labeling of I with 5 mg iodized C 60 -Dissolve 10mL of 0.5mM toluene in benzoic acid mustard, take 0.5mL and put it in an ampoule tube, add 20μL of Na 125 I solution (10 microcuries), seal the ampoule tube and place it in an oil bath at 130°C for 1 hour for isotope exchange; Developed on No. 1 filter paper, iodine-labeled C 60 -R for benzomustine f =0.9, 125 I- At the origin position, the marking rate reaches 9...
Embodiment 2
[0022] Example 2C 60 Inhibitory effect of -benzoic acid mustard on tumor cells in vitro
[0023] C 60 Preparation of aqueous solution 2.88mg C 60 (Fullerene) was dissolved in 100mL toluene, 90mg polyvinylpyrrolidone was dissolved in 100mL chloroform, and the two were mixed evenly, and the solvent was removed by rotary evaporation, and the residue after solvent removal was dissolved in 10mL pure water to obtain light yellow C 60 PVP solution.
[0024] Preparation of benzaldehyde nitrogen mustard aqueous solution Dissolve 0.98mg of benzaldehyde nitrogen mustard in 100mL of absolute ethanol, 90mg of polyvinylpyrrolidone in 100mL of chloroform, mix the two evenly, and remove the solvent by rotary evaporation, and the residue after removing the solvent Dissolve it with 10 ml of pure water to obtain a colorless benzaldehyde nitrogen mustard PVP solution.
[0025] C 60 -Preparation of aqueous solution of benzoambucil with 3.976mg C 60 - Benzoambucil was dissolved in 100 mL of a...
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