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Title: Synthesis and Antiproliferative Activity of Novel Quercetin-1,2,3- Triazole Hybrids using the 1,3-Dipolar Cycloaddition (Click) Reaction
Authors: Carreiro, Elisabete
Costa, Ana
Antunes, Célia
Keywords: 1,2,3-triazole
Huisgen reaction
molecular hybridization
Issue Date: 8-Jun-2022
Publisher: Thieme
Abstract: Twenty-three new quercetin-1,2,3-triazole hybrids were synthesized in good to quantitative yields via Cu(I)-catalyzed azide- alkyne cycloaddition reaction under microwave irradiation. These new hybrids contain a 1,4-disubstituted 1,2,3-triazole ring at the 3-OH posi- tion of quercetin whilst the remaining hydroxyl groups were either pro- tected as methyl or benzyl groups or left unprotected. All the querce- tin-1,2,3-triazole hybrids I–IV were evaluated against REM-134 canine mammary cancer cell line, which is used as a translational model for hu- man breast cancer. These new analogues exhibit potent antiprolifera- tive activity against this cancer cell line. Furthermore, the results show that some of the new quercetin-1,2,3-triazole hybrids have better activ- ity than quercetin. Our best inhibitors displayed IC50 values in the range of 41–180 nM, and undoubtedly will have an important impact on the treatment of both canine and human breast cancer.
Type: article
Appears in Collections:LAVQ-REQUIMTE - Publicações - Artigos em Revistas Internacionais Com Arbitragem Científica

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