Document type: | Patente |
Inventor(s): | Ricardo José Nunes; Alessandra Mascarello; Taisa Regina Stumpf; Paulo César Leal; José Andres Yunes; Carolina Pereira de Souza Melo; Rafael Renatino Canevarolo; Louise Domeneghini Chiaradia; Rosendo A. Yunes; Ângelo Bruneli Albertoni Laranjeira |
Applicant: | Universidade Federal de Santa Catarina (UFSC) |
Deposit date: | November 2012, 26 |
INPI register: |
The present invention relates to acyl-hydrazone compounds, in particular 3,4,5-trimethoxyphenyl-hydrazide derivatives, as well as the oxadiazole analogs thereof and other similar compounds, and to the pharmaceutical use of the same for the treatment of various diseases associated with cell proliferation, such as leukemias, including acute lymphoblastic leukemia (ALL), tumours and inflammation. Acyl-hydrazones have been obtained having activity similar to that of the compound used as a standard in experiments (colchicine). The greater selectivity of the compounds according to the invention is an important feature, associated with fewer side effects than the pharmaceuticals used at present in clinical treatments. The synthetised acyl-hydrazones, more particularly the compounds 02 and 07, exhibited important anti-leukemic activity, which suggests 02 and 07 as candidates to pharmaceutical prototypes, or to pharmaceuticals for the treatment of leukemias, in particular acute lymphoblastic leukemia (ALL), tumours and other proliferative diseases, such as inflammation. The action mechanism of the most active compounds was determined by using DNA microarrays and subsequent tests indicated by the chip, besides selectivity studies in healthy human lymphocytes
FAPESP's process: | 09/04167-1 - Metabolomics of methotrexate resistance in acute lymphoblastic leukemia |
Grantee: | Rafael Renatino Canevarolo |
Principal Investigator: | José Andrés Yunes |
Institution: | Centro Infantil de Investigações Hematológicas Dr Domingos A Boldrini (CIB) |
Support Opportunities: | Scholarships in Brazil - Master |
FAPESP's process: | 12/11952-0 - Methotrexate resistance is directly associated with glutathione concentration in acute lymphoblastic leukemia cell lines |
Grantee: | Rafael Renatino Canevarolo |
Principal Investigator: | José Andrés Yunes |
Institution: | Centro Infantil de Investigações Hematológicas Dr Domingos A Boldrini (CIB) |
Support Opportunities: | Scholarships in Brazil - Doctorate |
FAPESP's process: | 08/02106-2 - IGFBP7 role in chemotherapy resistance of Pediatric Acute Lymphoblastic Leukemia |
Grantee: | Angelo Brunelli Albertoni Laranjeira |
Principal Investigator: | José Andrés Yunes |
Institution: | Centro Infantil de Investigações Hematológicas Dr Domingos A Boldrini (CIB) |
Support Opportunities: | Scholarships in Brazil - Doctorate |
FAPESP's process: | 12/03039-2 - IGFBP7 and insulin/IGFs in Childhood Acute Lymphoblastic Leukemia chemoresistance |
Grantee: | Angelo Brunelli Albertoni Laranjeira |
Principal Investigator: | José Andrés Yunes |
Institution: | Centro Infantil de Investigações Hematológicas Dr Domingos A Boldrini (CIB) |
Support Opportunities: | Scholarships in Brazil - Post-Doctoral |
FAPESP's process: | 14/08247-8 - Preclinical studies of novel inhibitors of DNA methyltransferase in acute leukemia |
Grantee: | Nathalia Moreno Cury |
Principal Investigator: | José Andrés Yunes |
Institution: | Centro Infantil de Investigações Hematológicas Dr Domingos A Boldrini (CIB) |
Support Opportunities: | Scholarships in Brazil - Doctorate |