201666-94-6Relevant 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).
Total synthesis of (+)-azinothricin and (+)-kettapeptin
Hale, Karl J.,Manaviazar, Soraya,George, Jonathan H.,Walters, Marcus A.,Dalby, Stephen M.
supporting information; experimental part, p. 733 - 736 (2009/09/30)
(Chemical Equation Presented) Asymmetric total syntheses of (+)-azinothricin and (+)-kettapeptin have been completed through a common new pathway that exploits a highly chemoselective coupling reaction between the fully elaborated cyclodepsipeptide 5 and the glycal activated esters 3 and 4 at the final stages of both respective syntheses.
Asymmetric total synthesis of antitumour antibiotic A83586C
Hale, Karl J.,Cai, Jiaqiang
, p. 2319 - 2320 (2007/10/03)
The first asymmetric total synthesis of antitumour antibiotic A83586C has been accomplished.
