2. Academic Validation
  3. Design, synthesis, and biofunctional evaluation of novel pentacyclic triterpenes bearing O-[4-(1-piperazinyl)-4-oxo-butyryl moiety as antiproliferative agents

Design, synthesis, and biofunctional evaluation of novel pentacyclic triterpenes bearing O-[4-(1-piperazinyl)-4-oxo-butyryl moiety as antiproliferative agents

  • Bioorg Med Chem Lett. 2015 Oct 15;25(20):4500-4. doi: 10.1016/j.bmcl.2015.08.076.
Chun-Hui Zhao 1,  Cui-Li Zhang 2,  Jin-Jie Shi 1,  Xi-Yan Hou 3,  Bin Feng 4,  Long-Xuan Zhao 5
Affiliations

Affiliations

  • 1 Liaoning Normal University, School of Life Sciences, Liaoning Provincial Key Laboratory of Biotechnology and Drug Discovery, Dalian 116029, China.
  • 2 Dalian Medical University, Department of Biotechnology, Dalian 116044, China.
  • 3 Dalian Nationalities University, College of Life Science, Dalian 116600, China.
  • 4 Dalian Medical University, Department of Biotechnology, Dalian 116044, China. Electronic address: binfeng@dmu.edu.cn.
  • 5 Liaoning Normal University, School of Life Sciences, Liaoning Provincial Key Laboratory of Biotechnology and Drug Discovery, Dalian 116029, China; Liaoning Normal University, School of Chemistry and Chemical Engineering, Dalian 116029, China. Electronic address: lxzhao@lnnu.edu.cn.
PMID: 26343825 DOI: 10.1016/j.bmcl.2015.08.076
Abstract

A series of Pentacyclic Triterpenoids derivatives bearing O-[4-(1-piperazinyl)-4-oxo-butyryl moiety has been synthesized and investigated for their potential antiproliferative activities. Pentacyclic Triterpenoids derivative compounds were synthesized by a four or six step synthetic procedure. The activity studies were evaluated using Cell Counting Kit-8 method, and Western blotting analysis on A549 cells, MCF-7 cells and Hela cells. Compounds methyl 3-O-[4-(1-piperazinyl)-4-oxo-butyryl]olean-12-ene-28-oate (OA-4) and compound 2-O-[4-(1-piperazinyl)-4-oxo-butyryl]-3,23-dihydroxyurs-12-ene-28-oate (AA-5) were found to be promising antiproliferative agents. These compounds show potentiality for further optimization as antitumor drugs.

Keywords

Antiproliferative agent; Apoptosis; Cell cycle; Pentacyclic triterpenoid.

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