Synthesis of pyrrolo[2,3-d]pyrimidine derivatives and their antiproliferative activity against melanoma cell line

Myung Ho Jung, Hwan Kim, Won Kyoung Choi, Mohammed I. El-Gamal, Jin Hun Park, Kyung Ho Yoo, Tae Bo Sim, So Ha Lee, Daejin Baek, Jung Mi Hah, Jung Hyuck Cho, Chang Hyun Oh

    Research output: Contribution to journalArticlepeer-review

    50 Citations (Scopus)

    Abstract

    Synthesis of a new series of diarylureas and amides having pyrrolo[2,3-d]pyrimidine scaffold is described. Their in vitro antiproliferative activities against A375 human melanoma cell line and HS 27 fibroblast cell line were tested and the effect of substituents on pyrrolo[2,3-d]pyrimidine was investigated. The newly synthesized compounds, except N-acetyl derivatives (Id, Ie, and Im), generally showed superior or similar activity against A375 to Sorafenib. Among all of these derivatives, compounds Iq and Ir having imidazole and morpholine moieties, respectively, showed the most potent antiproliferative activity against A375.

    Original languageEnglish
    Pages (from-to)6538-6543
    Number of pages6
    JournalBioorganic and Medicinal Chemistry Letters
    Volume19
    Issue number23
    DOIs
    Publication statusPublished - 2009 Dec 1

    Bibliographical note

    Funding Information:
    We are grateful to the Korea Institute of Science and Technology (KIST) for financial support.

    Keywords

    • A375
    • Antiproliferative activity
    • HS 27
    • Melanoma
    • Pyrrolo[2,3-d]pyrimidine

    ASJC Scopus subject areas

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

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