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Title 

Synthesis and antitumor activity of natural compound aloe emodin derivatives

Authors 

N R ThimmegowdaChanmi ParkB ShwethaK SakchaisriK LiuJoonsung HwangSangku LeeSook-Jung JeongNak Kyun SoungJae-Hyuk JangIn Ja RyooJong Seog AhnR L EriksonBo Yeon Kim

Publisher 

John Wiley and Sons

Issue Date 

2015

Citation 

Chemical Biology and Drug Design, vol. 85, no. 5, pp. 638-644

Keywords 

aloe emodinaloe emodin derivativesantitumor activityHep G2 cellsNCI-H460 cellsstructure activity relationship

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.

ISSN 

1747-0277

Link 

http://dx.doi.org/10.1111/cbdd.12448

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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