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METHOD FOR THE PREPARATION OF 1,5-BIS(4-HYDROXY-3-METOXY-PHENYL)-PENTA-1,4-DIEN-3-ONE AND DERIVATIVES WITH ANTITUMORAL PROPERTIES 

Tipo de documento:Patente
Inventor(es): José Agustín Pablo Quincoces Suárez; Klaus Peseke; Marcus Kordian; João Ernesto de Carvalho; Luciana Konecny Kohn; Maria Aparecida Antônio; Heloiza Brunhari
Depositante: Academia Paulista Anchieta S/C Ltda (APA) ; Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) ; José Agustín Pablo Quincoces Suárez
Data do depósito: 28 de novembro de 2003
Registro INPI:
US12/307,669 - Consulta INPI
IPC: A61K 31/12 A61P 35/04
Resumo

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.sub.50, 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 (LD.sub.50 of 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.


Processo FAPESP: 99/09791-1 - Síntese de compostos premilados com potencial antimicrobiano e antitumoral
Beneficiário:José Agustín Pablo Quincoces Suárez
Pesquisador responsável:José Agustín Pablo Quincoces Suárez
Instituição: Universidade Bandeirantes (UNIBAN). Pró-Reitoria Acadêmica
Linha de fomento: Bolsas no Exterior - Pesquisa

Processo FAPESP: 01/10383-7 - Propriedades antitumorais da 1,5-bis(4-hidroxi-3-methoxi-fenil) penta-1,4-dien-3-ona e seus derivados
Beneficiário:José Agustín Pablo Quincoces Suárez
Pesquisador responsável:José Agustín Pablo Quincoces Suárez
Instituição: Universidade Bandeirantes (UNIBAN). Pró-Reitoria Acadêmica
Linha de fomento: Auxílio à Pesquisa - Programa de Apoio à Propriedade Intelectual (PAPI/Nuplitec)