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Synthesis of 2-amino-benzamide derivatives designed as fetal hemoglobin inducers

Grant number: 17/07789-0
Support Opportunities:Scholarships in Brazil - Scientific Initiation
Effective date (Start): October 01, 2017
Effective date (End): September 30, 2018
Field of knowledge:Health Sciences - Pharmacy
Principal Investigator:Jean Leandro dos Santos
Grantee:Gabriela Ribeiro Albuquerque
Host Institution: Faculdade de Ciências Farmacêuticas (FCFAR). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil


Sickle Cell Disease is a hematological disease characterized by a punctual mutation in the sixth codon of the ²-globin gene, responsible for the substitution of thymine for adenine (GAG to GTG). The discovery that butyrates promote increased production of fetal hemoglobin (HbF) by inhibiting histone deacetylases (HDACs) provides a new perspective of research on new drugs for treating this disease. Recent studies have demonstrated that inhibition of class I histone deacetylase (HDACs), mainly HDAC-1 and HDAC-2, causes increase in the production of HbF without causing changes in cell cycle and proliferation. Based on these advances, we propose in this project the synthesis of new HDAC-1 and HDAC-2 inhibitors potentially useful to treat the symptoms of sickle Cell Disease. (AU)

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Scientific publications
(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)
URIAS, BEATRIZ SILVA; PAVAN, ALINE RENATA; ALBUQUERQUE, GABRIELA RIBEIRO; PROKOPCZYK, IGOR MUCCILO; FERREIRA ALVES, TANIA MARA; FERREIRA DE MELO, THAIS REGINA; RODRIGUES SARTORI, GERALDO; MARTINS DA SILVA, JOAO HERMINIO; CHIN, CHUNG MAN; DOS SANTOS, JEAN LEANDRO. Optimization of Resveratrol Used as a Scaffold to Design Histone Deacetylase (HDAC-1 and HDAC-2) Inhibitors. PHARMACEUTICALS, v. 15, n. 10, p. 18-pg., . (18/11079-0, 17/07789-0, 18/19523-7, 15/19531-1, 15/21252-3, 19/09456-3)

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