کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1400085 | 1501239 | 2006 | 12 صفحه PDF | دانلود رایگان |
Several 1-alkyl-1,2,3,4-tetrahydroisoquinoline (TIQ) derivatives, which may play a role in Parkinson's disease, have been synthesized via Pummerer-type cyclization of the sulfonium ion formed in situ from N-formyl sulfoxide. Using an in vitro trypan blue exclusion assay, high concentrations of TIQ derivatives possessing bulky alkyl group substituents such as 1-cyclobutyl-, 1-cyclohexyl-, 1-phenyl- or 1-benzyl- at the C-1 position were found to significantly affect the viability of PC12 cells. Moreover, TIQ derivatives that moderately or strongly induced apoptosis (e.g., 1-phenyl-TIQ and 1-cyclohexyl-TIQ, respectively) paralleled the results obtained using the trypan blue exclusion assay. These results suggest that the size and electron-donating properties of functional groups may affect the cytotoxicity of TIQ derivatives.
1-Alkyl-1,2,3,4-tetrahydroisoquinoline (TIQ) derivatives, have been synthesized using Pummerer-type cyclization of sulfoxides, possessing bulky alkyl group at the C-1 position found to significantly affect the viability of PC12 cells.Figure optionsDownload as PowerPoint slide
Journal: European Journal of Medicinal Chemistry - Volume 41, Issue 2, February 2006, Pages 241–252