Synthesis and biological activity evaluation of emodin quaternary ammonium salt derivatives as potential anticancer agents - Details

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Abstract：

Twenty-six　emodin　derivatives　(17　novel)　which　attach　quaternary　ammonium　salt　were　synthesized　and　evaluated　for　their　anticancer　activities　in　vitro　and　in　vivo.　Compounds　11g　+　12g　and　11h　+　12h　had　more　significant　antiproliferative　ability　against　three　cancer　cell　lines　and　low　cytotoxicity　to　HELF.　11g　+　12g　and　11h　+　12h　induced　AGS　cell　apoptosis　and　arrested　cell　cycle　at　the　G0/G1　phase　in　a　dose-dependent　manner.　Furthermore,　the　activities　of　the　caspase-3,　-9　enzymes　were　increased　in　the　treated　cells.　In　vivo　studies　revealed　that　compounds　11g　+　12g　and　11h　+　12h　showed　significant　anti-tumor　activity　compared　with　controlled　group.　©　2012　Elsevier　Masson　SAS.　All　rights　reserved.

Keyword：

Anticancer activity; Apoptosis; Emodin derivatives; Quaternary ammonium salt

Community：

[ 1 ] [Wang, W.]Institute of Organic Chemistry, College of Chemistry and Chemical Engineering, Fuzhou University, Fujian 350108, China
[ 2 ] [Bai, Z.]Department of Pharmaceutical Engineering, College of Chemistry and Chemical Engineering, Fuzhou University, Fujian 350108, China
[ 3 ] [Zhang, F.]Institute of Organic Chemistry, College of Chemistry and Chemical Engineering, Fuzhou University, Fujian 350108, China
[ 4 ] [Wang, C.]Institute of Organic Chemistry, College of Chemistry and Chemical Engineering, Fuzhou University, Fujian 350108, China
[ 5 ] [Yuan, Y.]Institute of Organic Chemistry, College of Chemistry and Chemical Engineering, Fuzhou University, Fujian 350108, China
[ 6 ] [Shao, J.]Department of Pharmaceutical Engineering, College of Chemistry and Chemical Engineering, Fuzhou University, Fujian 350108, China

Reprint 's Address：

[Shao, J.]Department of Pharmaceutical Engineering, College of Chemistry and Chemical Engineering, Fuzhou University, Fujian 350108, China

Email：

sophia8762@yahoo.com.cn

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Source ：

European Journal of Medicinal Chemistry

ISSN： 0223-5234

Year： 2012

Volume： 56

Page： 320-331

3 . 4 9 9

JCR@2012

6 . 0 0 0

JCR@2023

JCR Journal Grade：1

CAS Journal Grade：2

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WoS CC Cited Count：

SCOPUS Cited Count： 32

ESI Highly Cited Papers on the List： 0 Unfold All

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30 Days PV： 0

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