Anti-tumor activity of novel biisoquinoline derivatives against breast cancers |
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| Affiliation: | 1. Department of Anatomy and Cell Biology, University of Florida, Gainesville, FL 32610, USA;2. Department of Chemistry, University of Florida, Gainesville, FL 32611-7200, USA;3. Research Institute for Solar and Sustainable Energies (RISE), School of Materials Science & Engineering, Gwangju Institute of Science and Technology, 123 Cheomdan-gwagiro, Buk-gu, Gwangju 500-712, Republic of Korea;1. GIGA Neurosciences, Research Group in Behavioral Neuroendocrinology, Neuroendocrinology unit, University of Liège, 15 Avenue Hippocrate (B36), 4000 Liège, Belgium;2. Center for Neurosciences (C4N), Department Pharmaceutical Chemistry, Drug Analysis and Drug Information (FASC), Vrije Universiteit Brussel, Laarbeeklaan 103, 1090 Brussels, Belgium;3. Department of Psychology, University of Maryland, 2141 Tydings Hall, College Park, MD 20742-7201, USA |
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| Abstract: | Breast cancer is classified into three groups according to its expression of hormone/growth factor receptors: (i) estrogen receptor (ER) and progesterone receptor (PR)-positive; (ii) human epidermal growth factor receptor 2 (HER2)-positive; and (iii) ER, PR, and HER2-negative (triple-negative). A series of methoxy-substituted biisoquinoline compounds have been synthesized as a potential chemotherapeutic agent for the triple-negative breast cancers which are especially challenging to manage. Structure activity relationship study revealed that rigid 6,6′-dimethoxy biisoquinoline imidazolium compound (1c, DH20931) exhibited the significant growth inhibitory effects on both triple-positive and triple-negative human breast cancer cell lines with IC50 in the range of 0.3–3.9 μM. The 1c (DH20931) is more potent than structurally related noscapine for growth inhibition of MCF7 cell line (IC50 = 1.3 vs 57 μM) and MDA-MB231 cell line (IC50 = 3.9 vs 64 μM). |
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| Keywords: | Breast cancer Biisoquinoline Noscapine MCF7 MDA-MB231 |
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