Novel bis-benzimidazole-triazole hybrids: anticancer study, in silico approaches, and mechanistic investigation
The data revealed the outperformance of 7a-g analogs over 4a-h one with very effective IC<sub>50</sub> values; 4-13 µg/mL compared to the reference drugs. Moreover, detailed mechanistic analyses showed potent Aurora-A Kinase expression for the most active analogs 7a and 7d exhibiting IC<sub>50</sub>; 3.5 and 5.3 over the control cells 8 ng/mL respectively. Additionally, based on their Aurora-A Kinase inhibitory activity, compound 7a was promising in apoptosis induction and cell cycle arrest. Molecular docking studies with Aurora-A Kinase revealed binding behaviors similar to the co-crystallized ligand sunitinib. Finally, this scaffold exhibits cytotoxic activity via apoptosis, enzyme downregulation, and suppression of cell division.
Authors
- Elsayed H. Eltamany (ORCID: https://orcid.org/0000-0002-9210-1647)
- Ateyatallah Aljuhani (ORCID: https://orcid.org/0000-0001-7305-8674)
- Mohammed Almaghrabi (ORCID: https://orcid.org/0000-0003-4929-7071)
- Mohamed Reda Aouad (ORCID: https://orcid.org/0000-0001-7018-6654)
- Ahmed K. B. Aljohani (ORCID: https://orcid.org/0000-0003-2332-1125)
- Ahmed T. A. Boraei (ORCID: https://orcid.org/0000-0003-3832-1275)
- Hany E. A. Ahmed (ORCID: https://orcid.org/0000-0001-8898-8452)
- Samir A. Salama (ORCID: https://orcid.org/0000-0002-5210-1781)
- Moataz A. Soliman (ORCID: https://orcid.org/0000-0003-2330-5889)
- Read Alghamdi
Institutions
- Suez Canal University (EG)
- Prince Sattam Bin Abdulaziz University (SA)
- Taif University (SA)
- Al-Azhar University (EG)
- Taibah University (SA)
- Al-Azhar University (ID)
Publication Details
- Journal
- Future Medicinal Chemistry
- Published
- 2024-12-13
- DOI
- https://doi.org/10.1080/17568919.2024.2437980
- Citations
- 11
- Primary Topic
- Synthesis and biological activity
- Type
- article
- Field-Weighted Citation Impact
- 2.75
Funders
- Taif University