• Title/Summary/Keyword: 1,3,4-Triarylpyrazole

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Design, Synthesis, and Preliminary Cytotoxicity Evaluation of New Diarylureas and Diarylamides Possessing 1,3,4-Triarylpyrazole Scaffold

  • Choi, Won-Kyoung;El-Gamal, Mohammed I.;Choi, Hong-Seok;Hong, Jun-Hee;Baek, Dae-Jin;Choi, Ki-Hang;Oh, Chang-Hyun
    • Bulletin of the Korean Chemical Society
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    • v.33 no.9
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    • pp.2991-2998
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    • 2012
  • A series of new diarylureas and diarylamides possessing 1,3,4-triarylpyrazole scaffold was synthesized and their in vitro antiproliferative activities against A375P human melanoma cell line and NCI-60 cell line panel were tested. Compounds 9, 11, 12, 14, and 17-21 showed superior potency against A375P to Sorafenib. Over the NCI-60 cancer cell line panel, compound 14 possessing a methoxy group, amide linker, and 4-chloro-3-(trifluoromethyl)phenyl terminal ring showed the highest potency and broad-spectrum anticancer activity. Compound 13 showed high selectivity towards leukemia subpanel over other cancer types.