• Title/Summary/Keyword: Diarylamide

Search Result 3, Processing Time 0.014 seconds

Synthesis of New Pyrimidinylaminobenzene Derivatives and Their Antiproliferative Activities against Melanoma Cell Line

  • Kim, Hee Jin;Oh, Chang-Hyun;Yoo, Kyung Ho
    • Bulletin of the Korean Chemical Society
    • /
    • v.34 no.8
    • /
    • pp.2311-2316
    • /
    • 2013
  • A series of new diarylamide and diarylurea derivatives possessing pyrimidinylaminobenzene scaffold was synthesized. Their in vitro antiproliferative activities were tested against A375P human melanoma cell line. Among them, compounds 1a-c, k and 2b-d, f, g, j, l showed superior potencies against A375P human melanoma cell line to Sorafenib. In particular, compound 2f possessing 3-fluoro-5-trifluoromethyl moiety exhibited the highest potency with $IC_{50}$ value in nanomolar scale.

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
    • /
    • v.33 no.9
    • /
    • pp.2991-2998
    • /
    • 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.

Optimization of the Reaction Conditions for Synthesis of 3-(Aryloxy)quinoline Derivatives via Friedländer's Cyclization Reaction

  • Khan, Mohammad Ashrafuddin;El-Gamal, Mohammed I.;Oh, Chang-Hyun
    • Bulletin of the Korean Chemical Society
    • /
    • v.34 no.6
    • /
    • pp.1848-1852
    • /
    • 2013
  • 6,7-Dimethoxy-2-methyl-3-(4-nitrophenoxy)quinoline was synthesized by Friedl$\ddot{a}$nder's cyclization reaction. Different bases and solvents were tested in order to optimize the reaction conditions. The highest yields were obtained using piperidine in refluxing ethanol. Further reactions were carried out in order to prepare different diarylamide and diarylurea derivatives in moderate to high yields in order to examine their anticancer activities.