| RRC ID |
64901
|
| 著者 |
Iqbal J, Saeed A, Shah SJ, al-Rashida M, Shams-ul Mahmood.
|
| タイトル |
Biological Evaluation of Azomethine-dihydroquinazolinone Conjugates as Cancer and Cholinesterase Inhibitors.
|
| ジャーナル |
Med Chem
|
| Abstract |
In an attempt to discover novel anti-cancer agents and potent cholinesterase inhibitors, 11 azomethine-dihydroquinazolinone conjugates were evaluated against lung carcinoma cells and cholinesterases. Most of the compounds exhibited significant cytotoxicity at low micromolar concentrations and were less toxic to normal cells. After 24 h incubation period, 2i showed maximum cytotoxicity. The 4-bromine substituted compounds showed higher acetylcholinesterase (AChE) inhibitory activity than other screened compounds. The most active compound 2c, among the series, had an IC50 value 209.8 µM against AChE. The tested compounds showed less inhibition against butyrylcholinesterase. Molecular docking studies were performed in order to investigate the plausible binding modes of synthesized compounds. The compounds can be further optimized to treat cancer and Alzheimer's disease. These derivatives may open new pathways for introducing new therapies for curing cancer and senile dementia.
|
| 巻・号 |
12(1)
|
| ページ |
74-82
|
| 公開日 |
2016-1-1
|
| DOI |
10.2174/1573406411666150708111417
|
| PII |
MC-EPUB-68657
|
| PMID |
26152145
|
| MeSH |
Acetylcholinesterase / metabolism
Alzheimer Disease / drug therapy
Animals
Antineoplastic Agents / chemical synthesis
Antineoplastic Agents / pharmacology*
Butyrylcholinesterase / metabolism
Cell Line, Tumor
Cholinesterase Inhibitors / chemical synthesis
Cholinesterase Inhibitors / pharmacology*
Drug Screening Assays, Antitumor
Horses
Humans
Hydrazones / chemical synthesis
Hydrazones / pharmacology*
Molecular Docking Simulation
Quinazolinones / chemical synthesis
Quinazolinones / pharmacology*
|
| IF |
2.577
|
| リソース情報 |
| ヒト・動物細胞 |
HCE-T(RCB2280) |
