Preprint Essay Version 2 This version not peer reviewed

Synthesis and Anti-Tumor Activity of Oleanolic Acid Derivatives

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. Preprints 2017, 2017040120 (doi: 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 (doi: 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 4, exhibited more potent cytotoxicity than positive drugs.

Subject Areas

oleanolic acid derivatives; synthesis; anti-tumor activity; molecular docking; computer-aided drug design

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