作者: Cohan Huxley , Mario Wibowo , Kah Yean Lum , Shelly Gordon , Sebastian D'Hyon
DOI: 10.1016/J.PHYTOCHEM.2020.112478
关键词:
摘要: Large-scale extraction of the leaves Australian rainforest tree Maytenus bilocularis followed by extensive purification studies afforded targeted and abundant dihydro-β-agarofuran, bilocularin A, in sufficient quantities (>500 mg) for detailed semi-synthetic chemistry. Eight A carbamate analogues were synthesised using a series commercially available isocyanate reagents high purity (>95%) variable yields (9-91%). All previously undescribed spectroscopically characterised NMR, UV, IR MS data. One compound crystalline material subsequent single crystal X-ray analysis (Cu-Kα) confirmed chemical structure along with absolute configuration. compounds evaluated anti-proliferative activity against human prostate cancer cell line LNCaP; none showed significant (>50%) growth inhibition at 20 μM. Compounds also tested their ability to inhibit leucine transport LNCaP cells, two moderate IC50 values 8.9 8.5 μM. This is first reported synthesis dihydro-β-agarofuran derivatives.