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.

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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

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article

Design, synthesis, and multitarget evaluation of thiosemicarbazone–sulfonamide hybrids as potent cholinesterase and MAO-A inhibitors with neuroblastoma-associated cytotoxicity

Nadeem Raza, Mostafa E. Salem, Rima D. Alharthy, Asif Rasool et al.
Scientific Reports
Enzyme function and inhibition
article

Design, synthesis, and multitarget evaluation of thiosemicarbazone–sulfonamide hybrids as potent cholinesterase and MAO-A inhibitors with neuroblastoma-associated cytotoxicity

Nadeem Raza, Mostafa E. Salem, Rima D. Alharthy, Asif Rasool, Zahid Shafiq, Mohamed Rahmtalla Elamin, Feyzi Sinan Tokalı, Khawar Abbas, Halil Şenol, Parham Taslimi, Furkan Çakır
article en

Abstract

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.

Scientific Reports
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)
Al-Imam Muhammad Ibn Saud Islamic University
Openalex Percentile: Top 10%
Enzyme function and inhibition
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Design, synthesis, and multitarget evaluation of thiosemicarbazone–sulfonamide hybrids as potent cholinesterase and MAO-A inhibitors with neuroblastoma-associated cytotoxicity — Nadeem Raza, Mostafa E. Salem, et al. · Scientific Reports (2026) | TGRS Research Map | TGRS