Version 1
: Received: 17 April 2017 / Approved: 19 April 2017 / Online: 19 April 2017 (05:00:30 CEST)
Version 2
: Received: 24 April 2017 / Approved: 24 April 2017 / Online: 24 April 2017 (12:08:36 CEST)
How to cite:
ZhenYu, K.; Li, L.; Zhan, S.; Li, C.; Zhao, Y.; Chen, H.; Meng, Y. Synthesis and Anti-Tumor Activity of Oleanolic Acid Derivatives. Preprints2017, 2017040120. https://doi.org/10.20944/preprints201704.0120.v2
ZhenYu, K.; Li, L.; Zhan, S.; Li, C.; Zhao, Y.; Chen, H.; Meng, Y. Synthesis and Anti-Tumor Activity of Oleanolic Acid Derivatives. Preprints 2017, 2017040120. https://doi.org/10.20944/preprints201704.0120.v2
ZhenYu, K.; Li, L.; Zhan, S.; Li, C.; Zhao, Y.; Chen, H.; Meng, Y. Synthesis and Anti-Tumor Activity of Oleanolic Acid Derivatives. Preprints2017, 2017040120. https://doi.org/10.20944/preprints201704.0120.v2
APA Style
ZhenYu, K., Li, L., Zhan, S., Li, C., Zhao, Y., Chen, H., & Meng, Y. (2017). Synthesis and Anti-Tumor Activity of Oleanolic Acid Derivatives. Preprints. https://doi.org/10.20944/preprints201704.0120.v2
Chicago/Turabian Style
ZhenYu, K., Hongrong Chen and Yanqiu Meng. 2017 "Synthesis and Anti-Tumor Activity of Oleanolic Acid Derivatives" Preprints. https://doi.org/10.20944/preprints201704.0120.v2
Abstract
Using the techniques of computer-aided drug design, the docking of Survivin and known active small molecules was simulated and then the key amino acid residue fragment of the target protein was analyzed. It led to the discovery of active groups capable of binding to the critical sites. Through the use of the natural product, Oleanolic Acid, as a lead compound, the introduction of the active groups onto the A-ring, and the modification of the carboxyl group at the C-28 position using esterification or amidation, twenty new Oleanolic acid derivatives had been designed and synthesized.A549 and SGC-7901 cells were used to screen the antitumor activity in vitro through the standard MTT method. The compounds, II3, III5 and Ⅳ4, exhibited more potent cytotoxicity than positive drugs.
Chemistry and Materials Science, Medicinal Chemistry
Copyright:
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
