Scholarship 23/13499-5 - Antineoplásicos, Compostos híbridos - BV FAPESP
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Synthesis and biological evaluation of purine-benzohydroxamates as potential inhibitors of PI3K and HDAC6 for the treatment of hematologic malignancies

Grant number: 23/13499-5
Support Opportunities:Scholarships in Brazil - Scientific Initiation
Start date until: December 01, 2023
End date until: November 30, 2024
Field of knowledge:Health Sciences - Pharmacy
Principal Investigator:Roberto Parise Filho
Grantee:João Pedro Freitas Verotti
Host Institution: Faculdade de Ciências Farmacêuticas (FCF). Universidade de São Paulo (USP). São Paulo , SP, Brazil

Abstract

Several studies pointed out the advantages of the multi-target approach in cancer treatment. In this context, the hybridization of pharmacophoric groups with distinct action can be a valuable strategy in the discovery of molecules capable of inhibiting two - or more - cellular signaling pathways, increasing the efficacy, and improving the therapeutic regimen of chemotherapy treatment. Phosphoinositide 3-kinase (PI3K) and histone deacetylase 6 (HDAC6) inhibitors, when used in combination, have shown synergism of action and increased antineoplastic efficacy, especially in hematological tumors. Herein, this project aims the design and synthesis of hybrid dual-action PI3K´-HDAC6 inhibitors, as well as the biological evaluation against a panel of hematological and solid tumors.

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