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Title 

Exploration of isosteric replacement of imidazolidinone motif in 4-phenyl-1-arylsul-fonylimidazolidinone with pyrazole and pyrazolidinone for cytotoxicity

Authors 

S SubramanianV K SharmaJi Eun YunS H Jung

Publisher 

The Korean Chemical Society

Issue Date 

2014

Citation 

Bulletin of the Korean Chemical Society, vol. 35, no. 10, pp. 2922-2928

Keywords 

ArylsulfonylimidazolidinoneCytotoxicityPyrazolidinonesPyrazolones

Abstract 

To investigate the possible isosteric replacement of imidazolidinone moiety in 4-phenyl-1-arylsulfonyl-imidazolidinones (2) for broad and potent anti-cancer agents, a series of 5-phenyl-1H-pyrazol-3-yl 1-(acyl)indoline-5-sulfonates (4) and 1-(1-(acyl)indolin-5-ylsulfonyl)-5-phenylpyrazolidin-3-ones (5) were prepared and evaluated for their cytotoxicity against six human cancer cell lines. Although the pyrazoles 4 or pyrazolidinones 5 showed relatively good activity, still they showed lesser activity in comparison to imidazolidinones 2. These activity decreases could be interpreted with the effect of change of the hydrogen bonding characteristics and the substitution pattern on structural variations of five membered rings from imidazolidinones 2 to pyrazoles 4 and pyrazolidinones 5, respectively. Therefore, it can be concluded that 4-phenyl-1-arylsulfonylimidazolidinone is a basic pharmacophore of imidazolidinones 2.

ISSN 

0253-2964

Link 

http://dx.doi.org/10.5012/bkcs.2014.35.10.2922

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


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