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This research aims to evaluate novel triaryl-tethered acryloyl derivatives as β-tubulin inhibitors effective in treating hepatocellular carcinoma.

May 2, 20260 citations

Design, Green Synthesis, and Biological Evaluation of Novel Triaryl-Tethered Acryloyl Derivatives as New Generation β-Tubulin Inhibitors for Hepatocellular Carcinoma Treatment.

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AAAamal A. Al‐Mutairi MMMai A E Mourad AAArwa Sultan Alqahtani

Key Points

This research aims to evaluate novel triaryl-tethered acryloyl derivatives as β-tubulin inhibitors effective in treating hepatocellular carcinoma.
Designed and synthesized novel triaryl-tethered acryloyl derivatives.
Evaluated the effects of compound 4i on apoptosis and cell cycle progression at G2/M phase.
Performed molecular docking studies to assess inhibitory activities.
Compound 4i induced apoptosis and halted cell cycle progression at G2/M phase.
Downregulation of Bcl-2 and upregulation of Bax and caspase 9 were observed, indicating apoptosis activation.
Molecular docking confirmed the inhibitory activities of the synthesized compounds.

Abstract

= 4.45 µM). Further studies revealed the ability of the promising compound 4i to induce apoptosis and halt the cellular cycle at G2/M phase. Furthermore, the apoptosis-inducing activity of naphthalene-tethered acryloyl moiety 4i was correlated to the downregulation of Bcl-2 as well as elevation of both Bax and caspase 9 as concluded from RT-PCR immunoassay measurements. Finally, molecular docking studies were also performed to explain the displayed inhibitory activities.

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Al‐Mutairi et al. (Fri,) studied this question.

synapsesocial.com/papers/69f5951171405d493affffdc https://doi.org/https://doi.org/10.1002/ddr.70303

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