Synthesis and antitumor activity of natural compound aloe emodin derivatives

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Title
Synthesis and antitumor activity of natural compound aloe emodin derivatives
Author(s)
N R Thimmegowda; Chanmi Park; B Shwetha; K Sakchaisri; K Liu; Joonsung Hwang; Sangku Lee; Sook-Jung Jeong; Nak Kyun SoungJae-Hyuk Jang; In Ja Ryoo; Jong Seog Ahn; R L Erikson; Bo Yeon Kim
Bibliographic Citation
Chemical Biology & Drug Design, vol. 85, no. 5, pp. 638-644
Publication Year
2015
Abstract
In this study, we have synthesized novel water soluble derivatives of natural compound aloe emodin 4(a-j) by coupling with various amino acid esters and substituted aromatic amines, in an attempt to improve the anticancer activity and to explore the structure-activity relationships. The structures of the compounds were determined by 1H NMR and mass spectroscopy. Cell growth inhibition assays revealed that the aloe emodin derivatives 4d, 4f, and 4i effectively decreased the growth of HepG2 (human liver cancer cells) and NCI-H460 (human lung cancer cells) and some of the derivatives exhibited comparable antitumor activity against HeLa (Human epithelial carcinoma cells) and PC3 (prostate cancer cells) cell lines compared to that of the parent aloe emodin at low micromolar concentrations. In the present study we have synthesized natural compound aloe emodin derivatives 4(a - j) to improve the anticancer activity and to explore the structure-activity relationships. Cell growth inhibition assays revealed that the aloe emodin derivatives 4d, 4f and 4i effectively decreased the growth ofHepG2 (human liver cancer cells), NCI-H460 (human lung cancer cells) and some of the derivatives exhibited comparable antitumor activity against HeLa (Human epithelial carcinoma cells) and PC3 (prostate cancer cells) cell lines compared to that of the parent aloe emodin at low micro molar concentrations.
Keyword
Hep G2 cellsNCI-H460 cellsantitumor activitystructure activity relationshipaloe emodinaloe emodin derivatives
ISSN
1397-002X
Publisher
Wiley
DOI
http://dx.doi.org/10.1111/cbdd.12448
Type
Article
Appears in Collections:
Ochang Branch Institute > Chemical Biology Research Center > 1. Journal Articles
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