6 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 invention discloses a podophyllotoxin structure-based tubulin / EGFR (epidermal growth factor receptor) dual-targeting podophyllotoxin triazole derivative and application thereof in antitumor drugs, and belongs to the technical field of medicinal chemistry. A triazole group is introduced into a podophyllotoxin mother nucleus through click chemistry, and a series of novel derivatives are designed and synthesized. Molecular docking studies show that the compound can target tubulin and EGFR kinase structural domains at the same time, and tumor cell proliferation is inhibited through a double-target synergistic effect. In-vitro experiments prove that the derivative has significant inhibitory activity on non-small cell lung cancer cells and has low toxicity on normal pulmonary epithelial cells. The dual-targeting strategy can overcome the drug resistance problem of the EGFR inhibitor, optimizes the pharmacokinetic characteristics, has the advantages of high oral availability, good in-vivo stability and the like, and is suitable for treatment of solid tumors such as non-small cell lung cancer and the like.

The invention discloses albumin-coupled prodrug nanoparticles as well as a preparation method and application thereof, and belongs to the technical field of medicines, a prodrug is a podophyllotoxin derivative, and the albumin-coupled prodrug nanoparticles stably exist in a normal physiological environment and specifically release a parent drug podophyllotoxin in tumor cells; the albumin-coupled podophyllotoxin prodrug nanoparticle can be efficiently accumulated at a tumor site in a tumor-bearing mouse, and has an outstanding anti-tumor curative effect on cell and animal levels, and a new strategy and more choices are provided for improving the defects of podophyllotoxin in clinical application and developing a functionalized nano-drug delivery system. And the method has a relatively great application prospect. # imgabs0 #

The present application relates to the field of pharmaceutical chemistry technology, and specifically discloses a podophyllotoxin derivative, its preparation method, and application. The general structural formula of the podophyllotoxin derivative is: wherein the general structural formula of R is: R1 is selected from one of CH3, (CH2)4CH3, citronellol, and piperonyl alcohol; X is selected from one of S, S-S, Se, O, C, and C-C; and n is 1 or 2. The podophyllotoxin derivatives in this application have good in vitro antitumor activity, specifically releasing or accumulating drugs in the tumor environment to achieve low-toxicity, high-efficiency, targeted tumor treatment.

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.