Scholarship 24/04316-7 - Hibridação molecular - BV FAPESP
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Purino-benzo-hydroxamates bearing acrylamide warhead: Synthesis and biological evaluation of covalent inhibitors for the treatment of hematologic neoplasms

Grant number: 24/04316-7
Support Opportunities:Scholarships in Brazil - Scientific Initiation
Start date until: June 01, 2024
End date until: May 31, 2025
Field of knowledge:Health Sciences - Pharmacy
Principal Investigator:Roberto Parise Filho
Grantee:Juliana Lefone Bessa
Host Institution: Faculdade de Ciências Farmacêuticas (FCF). Universidade de São Paulo (USP). São Paulo , SP, Brazil

Abstract

Cancer, a complex disease, requires innovative treatment strategies, such as multi-target therapy, which seeks to maximize therapeutic efficacy by simultaneously attacking multiple biological targets. In this context, the focus on hybrid inhibitors, capable of acting on several targets and enhancing synergistic effects, has been gaining prominence, especially in the inhibition of HDACs and kinases, which are crucial in the development of neoplasms. In our group, Lapessb, we have developed hybrid inhibitors with significant antitumor activity in hematological neoplasms, demonstrating efficacy in the nanomolar range against HDACs and micromolar for JAK3. The current challenge focuses on improving the potency and selectivity of these inhibitors, especially through the incorporation of electrophilic warheads that allow covalent binding, especially with the JAK target, enhancing antitumor activity. This strategic modification aims not only to improve the efficacy of the compounds, but also their specificity, minimizing unwanted interactions. The designed compounds will be synthesized, characterized and subjected to biological tests on hematological neoplasm cells and, in addition, on the isolated targets.

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