Synthesis and antitumor activity of arylsubstituted imidazolin-2-one derivatives / 药学学报
Acta Pharmaceutica Sinica
; (12): 711-716, 2005.
Article
in Zh
| WPRIM
| ID: wpr-353423
Responsible library:
WPRO
ABSTRACT
<p><b>AIM</b>To design and synthesize new arylsubstituted imidazolin-2-one analogues as antitumor compounds.</p><p><b>METHODS</b>Arylsubstituted imidazolin-2-ones were prepared by condensation the appropriate omega-amino-acetophenone hydrochloride with arylisocyanate in toluene. The target compounds prepared in this study were tested for cytotoxicity against PC-3, A549, HO-8910, Hela, HL60, K562 and HL60R cancer cell lines, and mechanism of one of the products 4y was further evaluated with its mechanium.</p><p><b>RESULTS</b>Thirty-six new compounds were synthesized and confirmed by 1H NMR, MS and elemental analysis. One of the synthesized products, compound 4y, displayed an encouraging selective activity against HL60 cells, and it was partlydue to the cell cycle arrest and cell apoptosis.</p><p><b>CONCLUSION</b>Compound 4y is worthy to be intensively studied.</p>
Full text:
1
Index:
WPRIM
Main subject:
Pharmacology
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Molecular Structure
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Cell Cycle
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Chemistry
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Apoptosis
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HL-60 Cells
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Cell Line, Tumor
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Imidazolines
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Amides
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Imidazoles
Limits:
Humans
Language:
Zh
Journal:
Acta Pharmaceutica Sinica
Year:
2005
Type:
Article