The role of silicon in drug discovery: a review

Panayides, Jenny-Lee; Riley, Darren Lyall; Hasenmaile, Felix; van Otterlo, Willem A. L.

doi:10.1039/d4md00169a

RSC Med. Chem.

2024

DOI: 10.1039/d4md00169a

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The role of silicon in drug discovery: a review

Jenny-Lee Panayides,

Darren Lyall Riley,

Felix Hasenmaile

et al.

Abstract: This review aims to highlight the role of silicon in drug discovery.

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Cited by 5 publications

References 509 publications

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Development and characterization of sodium alginate and β-cyclodextrin nanoemulsions encapsulating betel leaf (Piper betle L.) extract for enhanced antimicrobial efficacy against foodborne pathogen

Aayush,

Singh,

Chiu

et al. 2025

Food Chemistry

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Development and characterization of sodium alginate and β-cyclodextrin nanoemulsions encapsulating betel leaf (Piper betle L.) extract for enhanced antimicrobial efficacy against foodborne pathogen

Aayush,

Singh,

Chiu

et al. 2025

Food Chemistry

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First Sila-Vitamin D Analogues: Design, Synthesis, Structural Analysis and Biological Activity

Loureiro,

Seoane,

Sampaio-Dias

et al. 2024

J. Med. Chem.

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The incorporation of silicon bioisosteres into pharmacological structures has been used as a strategy to improve the therapeutic potential of drugs. However, no secosteroidal silicon-containing VDR ligands have been developed. Here we report the design, synthesis, and biological activity of six analogues of the natural hormone 1,25-dihydroxyvitamin D3 (1,25D 3 ), which incorporate a silicon atom as a side chain-C25 isostere. The analogues were synthesized by the Wittig−Horner approach starting from Inhoffen-Lythgoe diol. The crystal structures of the complexes formed by the sila-analogues with the ligand binding domain of VDR revealed additional interactions of the silacontaining side chains that stabilize the VDR active conformation. These sila-analogues show similar VDR binding and transcriptional activity in comparison with the natural hormone 1,25D 3 , but with significantly less hypercalcemic activity. The new analogues, when combined with chemotherapy, significantly decrease cell proliferation.

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Organophotocatalytic Regioselective Silylation/Germylation and Cascade Cyclization of N-Alkenyl α-CF₃ Acrylamides: Access to Densely Functionalized 4-Pyrrolin-2-ones

Bajya,

Maurya,

Selvakumar

2024

Org. Lett.

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We report an organophotoredox-catalyzed silylation/germylation cascade cyclization of N-alkenyl α-CF 3 acrylamides under mild conditions. N-Aminopyridinium salts act as hydrogen atom transfer reagents under photoredox catalysis in the generation of silyl and germyl radicals. An array of silyl-and germyl-substituted 3-CF 3 -4-pyrrolin-2-one derivatives were constructed in a shorter reaction time with low catalyst loading in good to excellent yields at room temperature. Importantly, this protocol is amenable to the late-stage diversification of bioactive molecules, as well as to large-scale synthesis.

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The role of silicon in drug discovery: a review

Abstract: This review aims to highlight the role of silicon in drug discovery.

Cited by 5 publications

References 509 publications

Development and characterization of sodium alginate and β-cyclodextrin nanoemulsions encapsulating betel leaf (Piper betle L.) extract for enhanced antimicrobial efficacy against foodborne pathogen

Development and characterization of sodium alginate and β-cyclodextrin nanoemulsions encapsulating betel leaf (Piper betle L.) extract for enhanced antimicrobial efficacy against foodborne pathogen

First Sila-Vitamin D Analogues: Design, Synthesis, Structural Analysis and Biological Activity

Organophotocatalytic Regioselective Silylation/Germylation and Cascade Cyclization of N-Alkenyl α-CF₃ Acrylamides: Access to Densely Functionalized 4-Pyrrolin-2-ones

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The role of silicon in drug discovery: a review

Abstract: This review aims to highlight the role of silicon in drug discovery.

Cited by 5 publications

References 509 publications

Development and characterization of sodium alginate and β-cyclodextrin nanoemulsions encapsulating betel leaf (Piper betle L.) extract for enhanced antimicrobial efficacy against foodborne pathogen

Development and characterization of sodium alginate and β-cyclodextrin nanoemulsions encapsulating betel leaf (Piper betle L.) extract for enhanced antimicrobial efficacy against foodborne pathogen

First Sila-Vitamin D Analogues: Design, Synthesis, Structural Analysis and Biological Activity

Organophotocatalytic Regioselective Silylation/Germylation and Cascade Cyclization of N-Alkenyl α-CF3 Acrylamides: Access to Densely Functionalized 4-Pyrrolin-2-ones

Contact Info

Product

Resources

About

Organophotocatalytic Regioselective Silylation/Germylation and Cascade Cyclization of N-Alkenyl α-CF₃ Acrylamides: Access to Densely Functionalized 4-Pyrrolin-2-ones