Research Grants 21/08260-8 - Química farmacêutica, Antineoplásicos - BV FAPESP
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Design, synthesis and biological evaluation of hybrid inhibitors of phosphoinositide 3-kinases and histone deacetylase 6 for the treatment of hematologic malignancies

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. Moreover, the potency and selectivity will be verified against the isolated molecular targets. Computational studies will be conducted to better understand the interaction of these inhibitors with their biological targets and also drive the synthesis. (AU)

Articles published in Agência FAPESP Newsletter about the research grant:
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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)
VASSILIADES, SANDRA VALERIA; BORGES, LARA GIMENEZ; GIAROLLA, JEANINE; PARISE-FILHO, ROBERTO. Folate Pathway Inhibitors, An Underestimated and Underexplored Molecular Target for New Anti-tuberculosis Agents. MINI-REVIEWS IN MEDICINAL CHEMISTRY, v. 23, n. 17, p. 22-pg., . (21/08260-8, 17/00689-0)
WAITMAN, KAROLINE; PARISE-FILHO, ROBERTO. New kinase and HDAC hybrid inhibitors: recent advances and perspectives. Future Medicinal Chemistry, v. 14, n. 10, p. 22-pg., . (21/08260-8)

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