Synthesis and Biological Evaluation of Amidinourea and Triazine Congeners as Inhibitors of MDA-MB-231 Human Breast Cancer Cell Proliferation

Rosemary Bass, Sarah Jenkinson, Jennifer Wright, Tora Smulders-Srinivasan, Jamie C. Marshall, Daniele Castagnolo

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    Abstract

    A series of novel amidinourea derivatives was synthesized, and the compounds were evaluated as inhibitors of MDA-MB-231 human breast cancer cell proliferation. In addition, a second series of triazine derivatives designed as rigid congeners of the amidinoureas was synthesized, and the compounds were evaluated for their antiproliferative activity. Among the two series, amidinourea 3d (N-[N-[8-[[N-(morpholine-4-carbonyl)carbamimidoyl] amino]octyl]carbamimidoyl]morpholine-4-carboxamide) emerged as a potent anticancer hit compound with an IC50 value of 0.76 mm, similar to that of tamoxifen
    Original languageEnglish
    Pages (from-to)288-291
    JournalChemMedChem
    Volume12
    Issue number4
    Early online date11 Jan 2017
    DOIs
    Publication statusPublished - 20 Feb 2017

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