58 results about "Combretastatin" patented technology

The invention discloses a combretastatin compound and a preparation method. The preparation method of the combretastatin compound of the invention comprises the following steps: dissolving 3'-amino combretastatin and N-(1-oxyl-2,2,6,6,-tetramethyl-oxygen-carbonyl)-L-amino acid in dried dichloromethane, uniformly stirring under argon protection, adding dicyclohexylcarbodiimide and 1-hydroxybenzotriazole, stirring and reacting under argon protection, filtering and removing white precipitates after the reaction, removing the solvent by distillation to obtain a crude product, purifying the crude product by column chromatography, and eluting the product by petroleum ether and ethyl acetate liquid with a volume ratio of 10:1-5:1 to obtain the target product. The combretastatin compound of the invention is applicable to the preparation of anticancer medicaments, and is especially applicable to the preparation of medicaments for treating leukemia, liver cancer, gastric cancer, and cervical cancer.

Compounds are disclosed that are designed to mimic the activity of combretastatin A-4 based on chalcone, aurone, or indanone structures, or involving benzoquinone or quinone rings. The anti-cancer activity of exemplified compounds is demonstrated in a range of in vitro and in vivo assays.

The invention relates to a method for synthesizing and preparing antineoplastic Combretastatin A-1 phosphate ester tetrasodium salt, comprising the steps: under the anhydrous condition, Combretastatin A-1 is dissolved in aprotic polar solvent, and dialkyl oxyl phosphoryl chloride/bromine (chloride/bromine phosphoric acid when R1 and R2 are hydrogen atoms) is dipped into the solution when acid-binding agent exists for reaction, and water is added into the reaction solution for stopping the reaction when the reaction is finished; products are extracted by the aprotic polar solvent, and then is decompressed and concentrated until being dried, so that the Combretastatin A-1 phosphate ester is obtained; (2) the obtained Combretastatin A-1 phosphate ester is dissolved into polar organic solvent to remove R1 and R2 radicals, and then obtained product is salified with sodium methoxide, finally, the Combretastatin A-1 phosphate ester tetrasodium salt is obtained. The method has simple and convenient technique, high yield coefficient and utilization rate of the Combretastatin A-1, and low production cost.

This invention relates to methods for treating a hematopoietic neoplasm comprising administering a therapeutically effective amount of a combretastatin compound, or a pharmaceutically acceptable salt thereof, to a subject having a hematological malignancy, wherein the combretastatin compound comprises a catechol or quinone moiety and is capable of forming a reactive oxygen species (ROS) in vivo. The method may further comprise co-administering a second chemotherapeutic agent.

The invention discloses the application of a compound shown as a formula I or a formula II. The application is characterized in that the compound is used for preparing medicine for destroying tumor vessels.

The invention provides a preparation method of combretastatin furan type analogues. The preparation method of the combretastatin furan type analogues (A and C) comprises the following steps of adding a solvent 1, a compound P1 and 3,4,5-triethoxy benzaldehyde into a reaction flask; adding alkali while stirring; reacting for 10 minutes at room temperature; adding diluted acid to regulate pH (Potential of Hydrogen) to be neutral; obtaining the combretastatin furan type analogue C through separation and purification; obtaining a compound A by reducing the C in a solvent 2 by using Raney Ni. The preparation method of combretastatin furan type analogues (B and D) comprises the following steps of adding the solvent 1, a compound P2 and 3-trimethylsilyl ether-4-methoxybenzaldehyde into the reaction flask; adding alkali while stirring; reacting for 10 minutes at the room temperature; adding the diluted acid to regulate pH (Potential of Hydrogen) to be neutral; obtaining the combretastatin furan type analogue D through separation and purification; obtaining a compound B by reducing the D in the solvent 2 by using the Raney Ni. The preparation method of the combretastatin furan type analogues, provided by the invention, has the advantages that the yield is high, the operation is simple, the reaction conditions are moderate, the used solvents are cheap and easy to get, industrial production is easy to realize, and the like.

Combretastatin derivatives of formula (I), preparation and use thereof are disclosed, wherein: R_f is alkyl with 1-8 carbon atoms and 1-17 fluorine atoms, R is amino, substituted amino, hydroxyl, nitro, halo, alkyloxy, phosphate or amino acid side chain. Said derivatives have a capability to inhibit the polymerization of microtubules and are useful in treatment against tumor and neovascularization.