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[Synthesis and antitumor activity of arylsubstituted imidazolin-2-one derivatives].
- Source :
-
Yao xue xue bao = Acta pharmaceutica Sinica [Yao Xue Xue Bao] 2005 Aug; Vol. 40 (8), pp. 711-6. - Publication Year :
- 2005
-
Abstract
- Aim: To design and synthesize new arylsubstituted imidazolin-2-one analogues as antitumor compounds.<br />Methods: 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.<br />Results: 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.<br />Conclusion: Compound 4y is worthy to be intensively studied.
- Subjects :
- Amides chemistry
Amides pharmacology
Antineoplastic Agents chemistry
Antineoplastic Agents pharmacology
Apoptosis drug effects
Cell Cycle drug effects
Cell Line, Tumor
HL-60 Cells
Humans
Imidazoles chemistry
Imidazoles pharmacology
Imidazolines chemistry
Imidazolines pharmacology
Molecular Structure
Amides chemical synthesis
Antineoplastic Agents chemical synthesis
Imidazoles chemical synthesis
Imidazolines chemical synthesis
Subjects
Details
- Language :
- Chinese
- ISSN :
- 0513-4870
- Volume :
- 40
- Issue :
- 8
- Database :
- MEDLINE
- Journal :
- Yao xue xue bao = Acta pharmaceutica Sinica
- Publication Type :
- Academic Journal
- Accession number :
- 16268505