Issue 10, 2012
From the journal:

MedChemComm

Synthesis, anti-proliferative and proapoptotic activity of novel oleanolic acid azaheterocyclic derivatives†

Xiao Kang,‡a   Jun Hu,‡b   Zhenbei Gao,a   Yong Ju*b  and  Chuanlian Xu*a  

* Corresponding authors

a Lab of Prometics & Molecular Enzymology, College of Life Sciences, Zhejiang Sci-Tech University, Hangzhou 310018, China
E-mail: chuanlianxu@zstu.edu.cn
Tel: +86-571-86843566

b Key Lab. of Bioorganic Phosphorus Chemistry & Chemical Biology, Ministry of Education, Department of Chemistry, Tsinghua University, Beijing 100084, China
E-mail: juyong@tsinghua.edu.cn
Fax: +86-10-62781695

Abstract

Oleanolic acid (OA) derivatives with azaheterocyclic groups at the 2,3-positions of A ring were synthesized and their anti-proliferative effect and apoptosis induction abilities were determined in human hepatocellular carcinoma BEL-7404 cells. The results showed that compounds 4 and 5 with different azaheterocycle groups possessed better anti-proliferative activity than oleanolic acid. Meanwhile, their apoptosis induction and signal pathway were investigated which indicated that compound 4 significantly induced cell apoptosis through down-regulating Bcl-2 expression, up-regulating Bax expression, releasing cytochrome c and activating the caspase-3 pathway.

Graphical abstract: Synthesis, anti-proliferative and proapoptotic activity of novel oleanolic acid azaheterocyclic derivatives

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Article information

DOI
https://doi.org/10.1039/C2MD20051A
Article type
Concise Article
Submitted
21 Feb 2012
Accepted
06 Aug 2012
First published
07 Aug 2012

Med. Chem. Commun., 2012,3, 1245-1249

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Synthesis, anti-proliferative and proapoptotic activity of novel oleanolic acid azaheterocyclic derivatives

X. Kang, J. Hu, Z. Gao, Y. Ju and C. Xu, Med. Chem. Commun., 2012, 3, 1245 DOI: 10.1039/C2MD20051A

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