Publications by authors named "Floriano P S Junior"

Alpha-glucosidase inhibitors play an important role in Diabetes Mellitus (DM) treatment since they prevent postprandial hyperglycemia. The Glycoside Hydrolase family 13 (GH13) is the major family of enzymes acting on substrates containing α-glucoside linkages, such as maltose and amylose/amylopectin chains in starch. Previously, our group identified glycoconjugate 1H-1,2,3-triazoles (GCTs) inhibiting two GH13 α-glycosidases: yeast maltase (MAL12) and porcine pancreatic amylase (PPA).

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Imatinib mesylate was the first representative BCR-ABL1 tyrosine kinase inhibitor (TKI) class for the treatment of chronic myeloid leukemia. Despite the revolution promoted by TKIs in the treatment of this pathology, a resistance mechanism occurs against all BCR-ABL1 inhibitors, necessitating a constant search for new therapeutic options. To develop new antimyeloproliferative substances, we applied a medicinal chemistry tool known as molecular hybridization to design 25 new substances.

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Article Synopsis
  • The BCR-Abl-1 enzyme is crucial for treating chronic myeloid leukemia, and tyrosine kinase inhibitors like imatinib are used to inhibit it.
  • Researchers developed twelve new compounds using a specific chemical group and tested their effectiveness against leukemia cells and healthy cells to assess selectivity.
  • Three of these new compounds demonstrated significant inhibitory activity, showing potential to compete with imatinib for the same binding site on the BCR-Abl-1 enzyme.
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