Acetylene compound as well as preparation method and application thereof
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A technology for enediynes and compounds, which is applied in the field of new enediynes, can solve problems such as large limitations, limited application of enediynes, and no tumor cell selectivity, and achieve high biological activity.
Inactive Publication Date: 2014-08-13
EAST CHINA UNIV OF SCI & TECH
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In addition to synthesizing homologues of natural enediyne antibiotics, some of the artificially synthesized enediynes focus on photoinitiated reactions, which require ultraviolet light irradiation; some mainly form metal complexes, but they are limited
Although some enediynes can react under mild conditions, they are not selective for tumor cells and normal cells, which limits the application of enediynes in biological anti-tumor
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[0048] synthesis of enediyne a
[0049] The two raw materials used in the synthesis of enediyne a, 3,4-diiodo-N-benzylmaleimide and 3,3,3-triethoxy-1-propyne, were respectively based on literature Tetrahedron 2005 , 61, 4585 and Organic letters 2008 , 10, synthesized by the method described in 4915.
[0050]
[0051] Under nitrogen, copper iodide (98.5mg, 40mmol%), palladium acetate (29.2mg, 10mmol%), triphenylphosphine (68.2mg, 20mmol%), cesium carbonate (1.27g, 3.9mmol%) and 3 , 4-diiodo-N-benzylmaleimide (0.57g, 1.3mmol) was successively added to a dried Schlenk bottle, added tetrahydrofuran (4ml) and toluene (10ml) which had been distilled to remove water, and stirred, 3,3,3-Triethoxy-1-propyne (0.68g, 3.9mmol) was added, and the reaction was completed after stirring at 45°C for 5h. The crude solution of the reaction system was separated by column chromatography on a silicon-magnesium-type adsorbent with a eluent of cyclohexane / ethyl acetate=40:1, and after the solv...
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Abstract
The invention relates to a novel acetylene compound applied to an anti-cancer drug as well as a preparation method and application thereof. The invention provides an acetylene compound of which the structural formula is as shown in the specification, wherein R represents a functional group; R=R, CR1R2R3, (CR1R2)nX or NR1R2; R, R1, R2 and R3 are hydrogen, halogen, C1-C24 alkyl chains, an aromatic group and a heterocyclic group; n is 1-6; X is amino, an ether group, an amidogent, sulfydryl, phosphino, halogen or an ester group; the aromatic group is phenyl, naphthyl, pyrenyl, anthryl, alkyl or halogen; the heterocyclic group is pyrrole, thiophene, pyridine, piperazine, pyran, furfuran, imidazole, parazole or morpholine. The experiment proves that the acetylene can lead obvious chain interruption of DNA and apoptosis of tumor cells. The acetylene compound proves that the synthetic acetylene has high biological activity.
Description
technical field [0001] The invention relates to a novel enediyne compound which can be used for anticancer drugs, its preparation method and application. Background technique [0002] Cancer is one of the major diseases that cause human death. Clinically, the methods used to treat cancer include surgery, radiotherapy and chemotherapy to kill malignant tumor cells, among which chemotherapy is the main method. Commonly used therapeutic drugs are mainly antibiotics, such as doxorubicin, doxorubicin, paclitaxel, carboplatin, etc. These antibiotic drugs themselves also bring great toxic and side effects while treating cancer. Therefore, finding new anticancer drugs with low toxicity, high efficiency and high selectivity has always been a great challenge for scientists. [0003] Enediynes, as a novel anti-tumor antibiotic, have a unique molecular structure, anti-tumor mechanism and high-efficiency killing cells, and are by far the most active anti-tumor antibiotics. Such compou...
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