| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 2027667 | Steroids | 2016 | 8 Pages |
•13α-Estrones bearing different substituents at C-3 and C-17 were synthesized.•3-(N-Benzyltriazolylmethoxy)-13α-estrone proved to be potent on cancer cell lines.•Presence of the 17-keto or 17-OH functions is essential for substantial activity.
13α-Estrone derivatives containing various substituents on C-3 and C-17 were synthesized, and evaluated by means of MTT assays for in vitro antiproliferative activity against a panel of human adherent cancer cell lines (HeLa, MCF-7, A2780 and A431). Compounds with N-benzyltriazolylmethoxy moieties on C-3 proved to be more potent than their 3-hydroxy or 3-ether counterparts. Some triazoles exerted substantial cytostatic effects against particular tumor cell lines, with submicromolar IC50 values.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
