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Importance of Imidazolidinone Motif in 4-Phenyl-N-arylsulfonylimidazolidinone for their Anticancer Activity

  • Sharma, Vinay K. (College of Pharmacy and Institute of Drug Research and Development, Chungnam National University) ;
  • Lee, Ki-Cheul (College of Pharmacy and Institute of Drug Research and Development, Chungnam National University) ;
  • Joo, Cheon-Ik (College of Pharmacy and Institute of Drug Research and Development, Chungnam National University) ;
  • Sharma, Niti (College of Pharmacy and Institute of Drug Research and Development, Chungnam National University) ;
  • Jung, Sang-Hun (College of Pharmacy and Institute of Drug Research and Development, Chungnam National University)
  • Received : 2011.02.28
  • Accepted : 2011.04.25
  • Published : 2011.08.20

Abstract

To investigate the possible isosteric replacement of imidazolidinone moiety in 4-phenyl-N-arylsulfonylimidazolidinone for broad and potent anticancer agents, a series of 4-phenyl-l(N)-arylsulfonylimidazolidinones 6a-k, imidazolidinethione analogs 7a-i, and imidazolidine oxime analogs 8a-c were prepared and evaluated for their in vitro anticancer activity against four human cancer cell lines (human lung A549, human colon COLO205, human leukemia K562, human ovary SK-OV-3). Among all the derivatives of N-arylsulfonylimidazolidinone 6a-k, compounds 6f and 6g showed the best inhibition comparable to doxorubicin against all cancer cell lines. Increasing the carbon chain on alkyl moieties of carbamates as shown in 6c-g did not alter the activity. The imidazolidinethione analogs 7a-i and imidazolidin-2-one oxime derivatives 8a-c did not possess any good activity. Therefore, imidazolidinone moiety is the best pharmacophore among the 4-phenyl-Narylsulfonylimidazolidinone derivatives.

Keywords

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