Expanding the Inhibitory Potential of the Benzoxaborinine Scaffold against Carbonic Anhydrases: Synthesis, Structural Characterization, and Antitumor Activity.
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TL;DR
A series of 2H-benzoxaborinines synthesized via an "aromatic metamorphosis" strategy based on the nickel-catalyzed insertion of boron into benzofuran scaffolds were evaluated as novel carbonic anhydrase (CA) inhibitors and demonstrated superior antiproliferative activity against human triple-negative breast cancer and glioblastoma cancer cell lines.
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Enzyme function and inhibition
Ferrocene Chemistry and Applications
Magnetism in coordination complexes
A series of 2H-benzoxaborinines synthesized via an "aromatic metamorphosis" strategy based on the nickel-catalyzed insertion of boron into benzofuran scaffolds were evaluated as novel carbonic anhydra
APA
Gioele Renzi, L. Masoni, et al. (2026). Expanding the Inhibitory Potential of the Benzoxaborinine Scaffold against Carbonic Anhydrases: Synthesis, Structural Characterization, and Antitumor Activity.. Journal of medicinal chemistry, 69(6), 7414-7426. https://doi.org/10.1021/acs.jmedchem.6c00163
MLA
Gioele Renzi, et al.. "Expanding the Inhibitory Potential of the Benzoxaborinine Scaffold against Carbonic Anhydrases: Synthesis, Structural Characterization, and Antitumor Activity.." Journal of medicinal chemistry, vol. 69, no. 6, 2026, pp. 7414-7426.
PMID
41814644 ↗
Abstract 한글 요약
In this work, a series of 2-benzoxaborinines was synthesized via an "aromatic metamorphosis" strategy based on the nickel-catalyzed insertion of boron into benzofuran scaffolds and were evaluated as novel carbonic anhydrase (CA) inhibitors. All compounds were evaluated against seven human CA isoforms (I, II, IV, VA, VII, IX, and XII), with several derivatives displaying low-nanomolar inhibitory activity. X-ray crystallographic analysis of the complexes of 2-benzoxaborinine with hCA I and hCA II revealed significant differences compared with the 1-benzoxaborinine analogue, which can be attributed to the increased structural rigidity of the scaffold. Finally, the selected compounds (, , , and ) were further evaluated for their antiproliferative activity against human triple-negative breast cancer (MDA-MB-231) and glioblastoma (U87MG) cancer cell lines, with derivative demonstrating superior antiproliferative activity compared with the antitumor CA inhibitor SLC-0111.
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