New diarylureas and diarylamides possessing acet(benz)amidophenyl scaffold: Design, synthesis, and antiproliferative activity against melanoma cell line

Hee Jin Kim, Hye Jung Cho, Hwan Kim, Mohammed I. El-Gamal, Chang Hyun Oh, So Ha Lee, Taebo Sim, Jung Mi Hah, Kyung Ho Yoo

    Research output: Contribution to journalArticlepeer-review

    34 Citations (Scopus)

    Abstract

    A series of new diarylurea and diarylamide derivatives possessing acet(benz)amidophenyl scaffold was synthesized. Their in vitro antiproliferative activity was tested against A375P human melanoma cell line. Compounds 1c,d and 2c,d showed the highest potencies with IC 50 values in sub-micromolar scale. In addition, compounds 1b,e,l and 2e,l were more potent than Sorafenib but with IC 50 values in micromolar range. Moreover, compound 2c was equipotent to Vemurafenib, and 2d showed higher potency than Vemurafenib against A375P. Molar refractometry calculation and ADME profiling of the highest potent four derivatives 1c,d and 2c,d are also reported.

    Original languageEnglish
    Pages (from-to)3269-3273
    Number of pages5
    JournalBioorganic and Medicinal Chemistry Letters
    Volume22
    Issue number9
    DOIs
    Publication statusPublished - 2012 May 1

    Bibliographical note

    Funding Information:
    This research was supported by Korea Institute of Science and Technology (KIST) and Fundamental R&D Program for Core Technology of Materials funded by the Ministry of Knowledge Economy, Republic of Korea ( K0006028 ).

    Keywords

    • A375P
    • Acet(benz)amidophenyl
    • Antiproliferative activity
    • Diarylamide
    • Diarylurea
    • Melanoma

    ASJC Scopus subject areas

    • Biochemistry
    • Molecular Medicine
    • Molecular Biology
    • Pharmaceutical Science
    • Drug Discovery
    • Clinical Biochemistry
    • Organic Chemistry

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