2. Academic Validation
  3. Anti-tumor activity of novel biisoquinoline derivatives against breast cancers

Anti-tumor activity of novel biisoquinoline derivatives against breast cancers

  • Bioorg Med Chem Lett. 2014 Oct 15;24(20):4850-3. doi: 10.1016/j.bmcl.2014.08.053.
Aruna S Jaiswal 1,  Dimitri Hirsch-Weil 2,  Erick R Proulx 2,  Sukwon Hong 3,  Satya Narayan 4
Affiliations

Affiliations

  • 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 Department of Chemistry, University of Florida, Gainesville, FL 32611-7200, USA; 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. Electronic address: shong@gist.ac.kr.
  • 4 Department of Anatomy and Cell Biology, University of Florida, Gainesville, FL 32610, USA. Electronic address: snarayan@ufl.edu.
PMID: 25240616 DOI: 10.1016/j.bmcl.2014.08.053
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).

Keywords

Biisoquinoline; Breast cancer; MCF7; MDA-MB231; Noscapine.

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