5 results about "Colonic Carcinoma" patented technology

The application discloses a class of podophyllotoxin triazole ether derivatives, a preparation method and application thereof, belongs to the technical field of chemical pharmacy, and particularly relates to a class of podophyllotoxin triazole derivatives and application thereof in preparation of antitumor drugs. The application combines a triazole structure with a podophyllotoxin parent body by using a click chemistry reaction, designs and synthesizes a series of novel 1,2,3-triazole podophyllotoxin derivatives, optimizes the kinetic characteristics of the podophyllotoxin by introducing the triazole structure, and improves the anticancer effect and drug property. Molecular docking shows that the series of compounds have strong binding energy on AKT1 and tubulin, can target inhibit tubulin / AKT1, and in-vitro antitumor activity research shows that the molecules have strong inhibitory activity on the proliferation of human colon cancer cell strains, and can provide a new strategy for structural derivatization of podophyllotoxin.

A sesquiterpene acyl glycoside in rhizoma artemisiae japonicae and preparation method and application thereof. The present application belongs to the technical field of medicine, and relates to extraction and separation of a sesquiterpene acyl glycoside compound rhizoma artemisiae japonicae cembranoid I from rhizome of rhizoma artemisiae japonicae by using macroporous resin, silica gel and preparation chromatography and the like, and the preparation method is simple and easy to implement. 23 H 38 O 10 In vitro human cancer cell inhibition activity research shows that the compound has anticancer activity, including obvious inhibition on human colon cancer cells HT-29 and human breast cancer MCF-7 cells, and is expected to be developed into a new anticancer drug.

The invention discloses a benzo-aza compound as well as a preparation method and application thereof. The benzazepine compound and the pharmaceutically acceptable salt of the benzazepine compound prepared by the invention have relatively high sensitivity and very strong cytotoxic activity to human colon cancer cells HCT116 tumor cells. The triethylene diamine catalyst is adopted in the process of preparing the benzo-aza compound, the reaction conditions are relatively conventional, the reaction process is mild, simple and convenient, the operation is easy, the cost is low, and the method is suitable for industrial large-scale production; according to the method, various substrates are used as reactants, products with various and complex structures are obtained, the yield is high, and the application range of the method is widened. The compound prepared by the preparation method disclosed by the invention has relatively high cytotoxic activity on human colon cancer cells HCT116. Therefore, the preparation method provided by the invention can provide a basis for screening the benzazepine compound with good activity on tumor cells, and is beneficial to further screening out compounds with more excellent biological activity.

The application discloses a chiral imide derivative and a preparation method and application thereof. A simple synthesis method of NHC catalyzed imine and MBH carbonate is designed, and a chiral imide derivative is efficiently constructed by one-step method. Biological activity evaluation is carried out on the compounds, and the inhibition rates of all the compounds on three tumor cells, human lung cancer cells A549, human colon cancer cells LOVO and SW620, are enhanced with the increase of concentration, wherein, the compounds 3g, 3i, 3j and 3o show better inhibition effect on the three tumor cells, the inhibition rate of the compound 3g on the A549 cells reaches 50% at a concentration of 12.5 μg / ml, and the inhibition rates of the compounds 3i, 3j and 3o on the A549 cells are all above 70% at a concentration of 50.0 μg / ml, and the inhibition rate of the compound 3j on the A549 cells reaches 85.8%, so the compound 3j has the value of further development and research.

The present application relates to a kind of preparation of trifluoromethyl camptothecin compound and its use in antitumor drugs, the structural formula of the compound is shown as follows.In vitro cytotoxic activity screening results show that trifluoromethyl camptothecin compound has broad-spectrum antitumor activity, to human hepatocellular carcinoma cell (HepG2), human non-small cell lung cancer cell (A549), human colon cancer cell (SW480), human cholangiocarcinoma cell (QBC939), human breast cancer cell (MCF-7), human pancreatic cancer cell (PANC-1), human pancreatic cancer cell (BxPC-3) shows strong inhibitory activity.4 trifluoromethyl camptothecin compounds I, II, III, IV all show strong inhibition to the 7 tumor cell lines measured, IC 50 Value is 0.503-0.0112 μM, 4.8477-0.6516 μM, 1.825-0.0005 μM and 4.9043-0.4612 μM, all significantly better than control drug topotecan. Among them, the compound shows the strongest inhibitory activity to BxPC-3 cell line, IC 50 Value is in the range of 0.6516-0.0005 μM. Therefore, trifluoromethyl camptothecin compound is expected to be developed into a new antitumor drug.