Investigating biological activity spectrum for novel quinoline analogues

Bioorg Med Chem. 2007 Feb 1;15(3):1280-8. doi: 10.1016/j.bmc.2006.11.020. Epub 2006 Nov 14.


The lack of the wide spectrum of biological data is an important obstacle preventing the efficient molecular design. Quinoline derivatives are known to exhibit a variety of biological effects. In the current publication, we tested a series of novel quinoline analogues for their photosynthesis-inhibiting activity (the inhibition of photosynthetic electron transport in spinach chloroplasts (Spinacia oleracea L.) and the reduction of chlorophyll content in Chlorella vulgaris Beij.). Moreover, antiproliferative activity was measured using SK-N-MC neuroepithelioma cell line. We described the structure-activity relationships (SAR) between the chemical structure and biological effects of the synthesized compounds. We also measured the lipophilicity of the novel compounds by means of the RP-HPLC and illustrate the relationships between the RP-HPLC retention parameter logK (the logarithm of capacity factor K) and logP data calculated by available programs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antifungal Agents / chemical synthesis
  • Antifungal Agents / chemistry
  • Antifungal Agents / pharmacology*
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cell Proliferation / drug effects
  • Chlorella vulgaris / drug effects*
  • Chlorophyll
  • Chloroplasts / drug effects*
  • Chromatography, High Pressure Liquid
  • Electron Transport / drug effects
  • Humans
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Neuroectodermal Tumors, Primitive, Peripheral / drug therapy
  • Photosynthesis / drug effects
  • Quinolines / chemical synthesis
  • Quinolines / chemistry
  • Quinolines / pharmacology*
  • Spinacia oleracea / drug effects*
  • Structure-Activity Relationship
  • Tumor Cells, Cultured


  • Antifungal Agents
  • Antineoplastic Agents
  • Quinolines
  • Chlorophyll