Fundacao De Amparo a Pesquisa Do Estado De Sao Paulo

Luciana Konecny Kohn

José Agustin Quincoces Suárez

Klaus Peseke

Markus Kordian

João Ernesto Carvalho

Márcia Aparecida Antônio

Heloiza Brunhari

Marcus Kordian

José Agustin Quincoces Suarez

Márcia Aparecida Antonio

Joao Ernesto Carvalho

This patent of invention reports the method for the preparation of 1,5-bis(4-hydroxy-3-methoxyphenyl)-penta-1,4-dien-3-one and derivatives with antitumoral properties: the sample denominated 37 compound was obtained with high yield and purity with ultrasonic technique presenting cytostatic activity (growth inhibition) in the concentrations evaluated and cytotoxic activity (cellular death) from the concentration of 0.25 mg/mL against nine different types of human cancer cell lines. This compound has a LD, equals to 8.54 g/Kg. That means this product can be considered itself as practically nontoxic. Doxorubicin, anticarcinogen medicine used as reference in all these tests, is a product extremely toxic (LDof 20 mg/Kg) and it does not inhibit the growth of Mama NCI-ADR cell line (the one that expresses the phenotype of resistance against multiple drugs), therefore, out product presented a strong cytostatic activity. Other derivatives also presented a strong cytostatic activity, especially the one denominated EHB1 compound.

Method for the preparation of 1,5-bis(4-hydroxy-3-metoxy-phenyl)-penta-1,4-dien-3-one and derivatives with antitumoral properties

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Campinas, Brazil

Luciana Konecny Kohn