کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1397538 | 1501177 | 2011 | 8 صفحه PDF | دانلود رایگان |
A series of quinolino-benzo-[5, 6]-dihydroisoquindolium compounds (3a, 3f, 3g, and 3j) derived from alkaloid berberine were designed and synthesized as novel G-quadruplex ligands. Subsequent biophysical and biochemical evaluation demonstrated that the addition of pyridine ring and amino group into berberine improved the binding ability and selectivity towards G-quadruplex DNA in comparison with the previously reported 9-N-substituted berberine derivatives. Furthermore, qRT-PCR assay showed compound 3j led the down-regulation of c-myc gene transcription in leukemia cell line HL60, while little effect on normal cell line ECV-304, which was consistent with the behavior of an effective G-quadruplex ligand targeting c-myc oncogene.
A series of quinolino-benzo-[5, 6]-dihydroisoquindolium derivatives (3a, 3f, 3g, and 3j) was designed, synthesized and evaluated as new G-quadruplex ligands.Figure optionsDownload as PowerPoint slideHighlights
► A series of quinolino-benzo-[5, 6]-dihydroisoquindolium compounds derived from alkaloid berberine were synthesized.
► The addition of pyridine ring and amino group into berberine improved the binding ability and selectivity towards G-quadruplex DNA.
► Compound 3j led the down-regulation of c-myc gene transcription in leukemia cell line HL60, while little effect on normal cell line ECV-304.
Journal: European Journal of Medicinal Chemistry - Volume 46, Issue 5, May 2011, Pages 1906–1913