Adelaide Research & Scholarship
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https://hdl.handle.net/2440/68633
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| Type: | Journal article |
| Title: | Synthesis of A83586C analogs with potent anticancer and beta-catenin/TCF4/osteopontin inhibitory effects and insights into how A83586C modulates E2Fs and pRb |
| Author: | Hale, K. Manaviazar, S. Lazarides, L. George, J. Walters, M. Cai, J. Delisser, V. Bhatia, G. Peak, S. Dalby, S. LeFranc, A. Chen, Y. Wood, A. Crowe, P. Erwin, P. El-Tanani, M. |
| Citation: | Organic Letters, 2009; 11(3):737-740 |
| Publisher: | Amer Chemical Soc |
| Issue Date: | 2009 |
| ISSN: | 1523-7060 1523-7052 |
| Statement of Responsibility: | Karl J. Hale, Soraya Manaviazar, Linos Lazarides, Jonathan George, Marcus A. Walters, Jiaqiang Cai, Vern M. Delisser, Gurpreet S. Bhatia, S. Andrew Peak, Stephen M. Dalby, Amandine Lefranc, Ying-Nan P. Chen, Alexander W. Wood, Paul Crowe, Pauline Erwin and Mohamed El-Tanani |
| 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 beta-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). |
| Keywords: | Humans Depsipeptides DNA-Binding Proteins Transcription Factors Antineoplastic Agents Drug Screening Assays, Antitumor Inhibitory Concentration 50 E2F Transcription Factors E2F1 Transcription Factor beta Catenin Basic Helix-Loop-Helix Leucine Zipper Transcription Factors Transcription Factor 4 |
| Rights: | Copyright © 2009 American Chemical Society |
| DOI: | 10.1021/ol802818f |
| Published version: | http://dx.doi.org/10.1021/ol802818f |
| Appears in Collections: | Aurora harvest 5 Chemistry publications |
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