Anti-tumor activity of novel biisoquinoline derivatives against breast cancers

Aruna S. Jaiswal, Dimitri Hirsch-Weil, Erick R. Proulx, Sukwon Hong, Satya Narayan

Research output: Contribution to journalArticlepeer-review

3 Scopus citations

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).

Original languageEnglish (US)
Pages (from-to)4850-4853
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume24
Issue number20
DOIs
StatePublished - Oct 15 2014
Externally publishedYes

Keywords

  • Biisoquinoline
  • Breast cancer
  • MCF7
  • MDA-MB231
  • Noscapine

ASJC Scopus subject areas

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

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