[Synthesis and antitumor activity of arylsubstituted imidazolin-2-one derivatives].
OBJECTIVE
To design and synthesize new arylsubstituted imidazolin-2-one analogues as antitumor compounds.


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.


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.


CONCLUSIONS
Compound 4y is worthy to be intensively studied.
Cheng
Yun-feng
YF
School of Pharmaceutical Science, Zhejiang University, Hangzhou 310031, China.
Hu
Yong-zhou
YZ
He
Qiao-jun
QJ
D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D018922:HL-60 Cells; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D048288:Imidazolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure
C518117:3,4-diphenyl-imidazol-2-one-1-carboxylic acid phenyl amide; D000577:Amides; D000970:Antineoplastic Agents; D007093:Imidazoles; D048288:Imidazolines