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

= 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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Publication Details

Journal
Drug Development Research
Published
2026-04-30
DOI
https://doi.org/10.1002/ddr.70303
Primary Topic
Synthesis and biological activity
Type
article
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article

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

Islam Zaki, Aamal A. Al‐Mutairi, Arwa Sultan Alqahtani, Ayman Abo Elmaaty et al.
Drug Development Research
Synthesis and biological activity
article

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

Islam Zaki, Aamal A. Al‐Mutairi, Arwa Sultan Alqahtani, Ayman Abo Elmaaty, Mai A E Mourad
article en

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.

Drug Development ResearchVol. 87(3)
Imam Mohammad ibn Saud Islamic University (SA), Port Said University (EG)
Openalex Percentile: Top 14%
Synthesis and biological activity
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