• Archives of Pharmacal Research
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• v.25 no.4
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• pp.421-427
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• 2002

For probing the importance of planarity of imidazolidinone motif of 4-phenyl-1-(N-acylindoline-5-sulfonyl)imidazolidinones 1 for their cytotoxicity, 4-phenyl-1-(N-acylindoline-5-sulfonyl)[1,2,5]thiadiazolidine-1,1-dioxides 2 were prepared and their cytotoxicity were measured against human lung carcinoma (A549), human colon carcinoma (COLO205), human ovarian cancer (SK-OV-3), human leukemic cancer (K562), and murine colon adenocarcinoma (Colon26) cell lines in vitro. Although only carbonyl moiety of imidazolidinone ring was replaced with sulfonyl group, compounds 2 do not show any activity against all five cancer cell lines unlike 1. Therefore the planarity of imidazolidinone ring of 1 should be an important factor for their cytotoxic activity.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.344.3-345
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• 2002

For the development of novel anticancer agent. we have designed. synthesized. and tested novel 4-phenyl-1(N)-arylsulfonylimidazolidinones. As a result. much more potent cytotoxicities of these compounds against the various cancer cell lines than those of doxorubicin were demonstrated. Elaboration on aryl motif on sulfonyl moiety led us to find highly potent 4-phenyl-1-(N-acylindoline-5-sulfonyl)imidazolidinones. Among them, 4-phenyl-l- ［N-(p-aminobenzoyl)indoline-5-sulfonyl］imidazolidinone (PA) was proved to have good pharmacological profile. (omitted)