Preprint Essay Version 1 This version is not peer-reviewed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: Kuai, Z.; 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.v1). Kuai, Z.; 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.v1).

Abstract

With the computer drug-aided design and the key amino acid residue fragment of the target protein analyzed on the basis of simulated docking of Survivin and known active small molecules, the active groups capable of binding to the critical sites were determined. After the natural product Oleanolic acid was used as lead compound, then the active groups were introduced on the ring of A, next the carboxyl group at the C-28 position was modified by esterification or amidation, twenty new Oleanolic acid derivatives had been designed and synthesized. SKOV3 and BGC-823 cells were used to screen the antitumor activity in vitro through the standard MTT method. Among the selection, compounds II3、III5 and 4 exhibited more potent cytotoxicity than positive drugs.

Subject Areas

oleanolic acid derivatives; synthesis; anti-tumor activity; molecular docking

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