439292-95-2Relevant academic research and scientific papers
Synthesis of A83586C analogs with potent anticancer and β-catenin/TCF4/osteopontin inhibitory effects and insights into how A83586C modulates E2Fs and pRb
Hale, Karl J.,Manaviazar, Soraya,Lazarides, Linos,George, Jonathan,Walters, Marcus A.,Cai, Jiaqiang,Delisser, Vern M.,Bhatia, Gurpreet S.,Peak, S. Andrew,Dalby, Stephen M.,Lefranc, Amandine,Chen, Ying-Nan P.,Wood, Alexander W.,Crowe, Paul,Erwin, Pauline,El-Tanani, Mohamed
supporting information; experimental part, p. 737 - 740 (2009/09/27)
(Chemical Equation Presented) 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 β-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).
Synthetic route to the GE3 cyclodepsipeptide.
Hale, Karl J,Lazarides, Linos
, p. 1903 - 1906 (2007/10/03)
[reaction: see text] A reasonably efficient [2 + 2 + 2] fragment condensation strategy has been developed for assembling the cyclodepsipeptide sector of GE3 that involves 5-7. A Carpino HATU-mediated macrolactamization was used to close the 19-membered cy
