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

Research output: Contribution to journalArticle

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

Original languageEnglish
Pages (from-to)288-291
JournalChemmedchem
Volume12
Issue number4
Early online date23 Jan 2017
DOIs
Accepted/In press11 Jan 2017
E-pub ahead of print23 Jan 2017
Published20 Feb 2017

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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 3 d (N-[N-[8-[[N-(morpholine-4-carbonyl)carbamimidoyl]amino]octyl]carbamimidoyl]morpholine-4-carboxamide) emerged as a potent anticancer hit compound with an IC50value of 0.76 μm, similar to that of tamoxifen.

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