Design, synthesis, and multitarget evaluation of thiosemicarbazone–sulfonamide hybrids as potent cholinesterase and MAO-A inhibitors with neuroblastoma-associated cytotoxicity
of 5.23 µM and a selectivity index of 8.6 relative to HUVEC cells. Molecular docking and MM-GBSA analyses revealed strong binding affinities (docking scores - 10.4 to - 15.4 kcal/mol; ΔG_bind - 55.9 to - 88.4 kcal/mol), which were further supported by molecular dynamics simulations. DFT calculations indicated favorable electronic properties (HOMO-LUMO gap: 0.098-0.116 eV), while ADME predictions suggested acceptable drug-like behavior and good oral absorption. These results identify thiosemicarbazone derivative 5n as a promising multitarget lead for the development of agents targeting cholinergic dysfunction, MAO-A inhibition, and neuroblastoma proliferation.
Authors
- Nadeem Raza (ORCID: https://orcid.org/0000-0002-4433-8076)
- Mostafa E. Salem (ORCID: https://orcid.org/0000-0003-4341-410X)
- Rima D. Alharthy (ORCID: https://orcid.org/0000-0003-3165-929X)
- Asif Rasool (ORCID: https://orcid.org/0000-0003-2769-7568)
- Zahid Shafiq (ORCID: https://orcid.org/0000-0003-4088-8297)
- Mohamed Rahmtalla Elamin
- Feyzi Sinan Tokalı
- Khawar Abbas
- Halil Şenol
- Parham Taslimi
- Furkan Çakır
Institutions
- Bahauddin Zakariya University (PK)
- Kafkas University (TR)
- King Abdulaziz University (SA)
- Imam Mohammad ibn Saud Islamic University (SA)
- Bartin University (TR)
- Bezmiâlem Vakıf Üniversitesi (TR)
- Nanjing University (CN)
Publication Details
- Journal
- Scientific Reports
- Published
- 2026-05-11
- DOI
- https://doi.org/10.1038/s41598-026-52909-6
- Primary Topic
- Enzyme function and inhibition
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- Al-Imam Muhammad Ibn Saud Islamic University