Abstract
The synthesis of three potent new antitumor agents is described: the A83586C-citropeptin hybrid (1), the A83586C-GE3 hybrid (2), and l-Pro-A83586C (3). Significantly, compounds 1 and 2 function as highly potent inhibitors of ß-catenin/TCF4 signaling within cancer cells, while simultaneously downregulating osteopontin (Opn) expression. A83586C antitumor cyclodepsipeptides also inhibit E2F-mediated transcription by downregulating E2F1 expression and inducing dephosphorylation of the oncogenic hyperphosphorylated retinoblastoma protein (pRb).
Original language | English |
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Pages (from-to) | 737-740 |
Number of pages | 4 |
Journal | Organic Letters |
Volume | 11 |
Issue number | 3 |
DOIs | |
Publication status | Published - 05 Feb 2009 |
ASJC Scopus subject areas
- Biochemistry
- Organic Chemistry
- Physical and Theoretical Chemistry