| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1373319 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
Synthesis of seven semi-synthetic analogs of NDGA is described. An approach to NDGA derivatization is described in which the ortho-phenolic groups are tethered together by one atom, forming a 5-membered heterocyclic ring. The analogs were evaluated for cytotoxicity in four cancer cell lines and compared to NDGA and tetra-O-methyl-NDGA (M4N) (1a). NDGA bis-cyclic sulfate (2a), NDGA bis-cyclic carbonate (2b), and methylenedioxyphenyl-NDGA (2d) and NDGA tetra acetate (1b) showed anti-cancer activity in vitro. Two compounds, (1b) and (2b), were evaluated for anticancer activity in a mouse xenograft model of human melanoma and showed dose-dependent activity.
Graphical abstractNovel derivatives of nordihydoguaiaretic acid were synthesized and tested for in vitro and in vivo anticancer activity.Figure optionsDownload full-size imageDownload as PowerPoint slide
