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

Document type:Patente
Inventor(s): José Agustín Pablo Quincoces Suárez; Klaus Peseke; Marcus Kordian; João Ernesto de Carvalho; Luciana Konecny Kohn; Maria Aparecida Antônio; Heloiza Brunhari
Applicant: Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
Deposit date: November 2003, 08
INPI register:
PCT/BR2003/000177
IPC: C07C 49/248 C07C 49/255 C07C 67/08 C07C 45/71 C07C 45/74
Abstract

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 LD50, 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 (LD50 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 our product presented a strong cytostatic activity. Other derivatives also presented a strong cytostatic activity, specially the one denominated EHB1 compound.


Grantee:José Agustín Pablo Quincoces Suárez
Principal Investigator:José Agustín Pablo Quincoces Suárez
Institution: Universidade Bandeirantes (UNIBAN). Pró-Reitoria Acadêmica
Support Opportunities: Scholarships abroad - Research

Grantee:José Agustín Pablo Quincoces Suárez
Principal Investigator:José Agustín Pablo Quincoces Suárez
Institution: Universidade Bandeirantes (UNIBAN). Pró-Reitoria Acadêmica
Support Opportunities: Research Grants - Support for Intellectual Property Rights and Licensing (PAPI/Nuplitec)