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Title: Synthesis of Novel 1,2,3-Triazole-Dihyropyrimidinone Hybrids using Multicomponent 1,3-Dipolar Cycloaddition(Click)-Biginelli Reactions
Authors: Carreiro, Elisabete
Burke, Anthony
Sena, Ana Margarida
Padrón, José
Puerta, Adrián
Keywords: 1,2,3-triazole
Issue Date: 10-Jan-2020
Publisher: Thieme
Citation: Synlett, 2020, 31(06), 615-621
Abstract: Inthiswork,21novel(1,4-disubstituted1,2,3-triazole)-dihy- dropyrimidinone (1,2,3-trzl-DHPM) type hybrids were synthesized and characterized. These were divided into two types: hybrids A (5 in total) containing the dihydropyrimidinone heterocyclic ring decorated with a 1,4-disubstituted 1,2,3-triazole in the C-5 position [these compounds were accessed by a multicomponent copper(I)-catalyzed azide alkyne cycloaddition (CuAAC) (or click)–Biginelli reactions with satisfactory yields (39–57%)] and hybrids B (16 in total) containing two 1,2,3-tri- azole units in the C-5 and C-6 methyl position of the DHPM. Hybrids B were synthesized via functionalization of the C-6 methyl group of hy- brids A, a multistep sequence of reactions was used that included bro- mination, azidation, and a CuAAC. Hybrids B were obtained in very good to excellent yields (up to 99%). Some hybrids A and B were evalu- ated for their antiproliferative activity against different cancer cell lines that included A549 and SW1573 (non-small-cell lung), HBL-100 and T-47D (breast), HeLa (cervix) and WiDr (colon). Three of these hybrids were potent cell proliferation inhibitors of non-small-cell lung cancer, cervix cancer, breast cancer, and colon cancer.
Type: article
Appears in Collections:CQE - Publicações - Artigos em Revistas Internacionais Com Arbitragem Científica

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