Abstract
Using a phenotypic screening and SAR optimization approach, a phenyl-bis-oxazole derivative has beenidentified with anti-proliferative activity, optimized with the use of a panel of cancer cell lines. The leadcompound was synthesized by means of a short and effective two-step synthesis using Pd-catalyzeddirect arylation. The compound stabilizes several quadruplex DNA sequences including a human telomericDNA and one from the promoter of the HSP90 gene, although the structure–activity relationships of theseries are not obviously related to the quadruplex binding.
Lingua originale | English |
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pagine (da-a) | 5351-5355 |
Numero di pagine | 5 |
Rivista | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS |
Volume | 23 |
Stato di pubblicazione | Published - 2013 |
All Science Journal Classification (ASJC) codes
- ???subjectarea.asjc.1300.1303???
- ???subjectarea.asjc.1300.1313???
- ???subjectarea.asjc.1300.1312???
- ???subjectarea.asjc.3000.3003???
- ???subjectarea.asjc.3000.3002???
- ???subjectarea.asjc.1300.1308???
- ???subjectarea.asjc.1600.1605???