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Updated: May 14, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis and antiproliferative activity of C-3 functionalized isobenzofuran-1(3H)-ones
Róbson Ricardo Teixeira1, Gustavo Costa Bressan, Wagner Luiz Pereira
1Departamento de Química, Universidade Federal de Viçosa, Av. P.H. Rolfs, S/N, CEP 36.570-000, Viçosa, MG, Brazil. robsonr.teixeira@ufv.br
Abstract:
A series of thirteen C-3 functionalized isobenzofuran-1(3H)-ones (phtalides) was synthesized via condensation, aromatization, and acetylation reactions. NMR (one and two dimensional experiments), IR, and mass spectrometry analysis allowed confirmation of the identity of the synthesized compounds. The substances were submitted to in vitro bioassays against U937 (lymphoma) and K562 (myeloid leukemia) cancer cell lines using the MTT cytotoxicity assay. Some derivatives inhibited 90% of cell viability at 100 µM. Also, two phtalides presented biological activity superior than that of etoposide (VP16), a commercial drug used as a positive control in the assays. In silico drug properties of the evaluated compounds were calculated and the results are discussed.
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