Journal
CHEMICAL BIOLOGY & DRUG DESIGN
Volume 78, Issue 5, Pages 869-875Publisher
WILEY-BLACKWELL
DOI: 10.1111/j.1747-0285.2011.01215.x
Keywords
cytotoxicity assay; drug design; indole; piperazine; radio ligand binding assay; radioligands; sigma ligands
Funding
- Scientific & Technological Research Council of Turkey (TUBITAK) [108S009]
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To investigate the molecular features involved in sigma (sigma) receptors binding, a series of compounds based on indole scaffolds were synthesized and their chemical structures were confirmed by H-1-NMR, IR, and elemental analysis. Their affinity toward sigma(1) and sigma(2) receptor subtypes was evaluated. 1-{[4-(2-phenylethyl)piperazin-1-yl]methyl}-3-methyl-1H-indole 3b had a high affinity to sigma(1) receptors, while three compounds, 1-{3-[4-(substitutedphenyl)piperazin-1-yl]propyl}-1H-indole derivatives 4a-c had shown high affinity and selectivity for sigma(2) receptors. Cytotoxicity of the compounds was demonstrated on cancer cell lines from liver (HUH7), breast (MCF7), and colon (HCT-116) cancer cell lines. Compound 1c (3-{[4-(3,4-dichlorobenzyl)piperazin-1-yl]methyl}-1H-indole) showed significant cell growth inhibitory activity on the selected cancer cell lines.
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