3 results about "Podophyllotoxin derivatives" 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.

The present invention concerns a novel enantiomer of 9-(3-fluorophenyl)-5-(2- hydroxyethyl)-6,9-dihydro-[l,3]dioxolo[4,5-g]furo[3,4-b]quinolin-8(5H)-one (SU056), as well as pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising it, and its uses in medical treatments, particularly including cancer treatments.

The application discloses an indazole-nitrogen-substituted podophyllotoxin derivative, a synthesis method and application thereof, and belongs to the field of medicine. Different substituents, such as methyl, ethyl, propyl, benzyl, fluorine atom, chlorine atom, bromine atom, iodine atom and the like, are introduced into 1 and 3 positions of indazole podophyllotoxin to obtain a podophyllotoxin derivative shown in formula (V) with significantly improved antitumor activity. In vitro tumor cell activity inhibition experiments show that the antitumor activity of the compound shown in formula (V) is significantly improved compared with that of podophyllotoxin.