Document Detail


The synthesis and anti-proliferative effects of beta-elemene derivatives with mTOR inhibition activity.
MedLine Citation:
PMID:  16617020     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Fourteen beta-elemene derivatives containing a piperazine, a morpholine, a tetrahydropyrrole, a thiophenylethylamine, or a cyclohexamine group were synthesized. The structures of these beta-elemene derivatives were characterized with IR, 1H NMR, MS, and elemental analyses. All these derivatives had an increased anti-proliferative activity in human cervix epitheloid carcinoma HeLa, gastric carcinoma SGC-7901, and leukemia K562 cells comparing with that of beta-elemene. Among these derivatives, 13,14-bis(cis-3,5-dimethyl-1-piperazinyl)-beta-elemene (IIi), 13,14-bis[2-(2-thiophenyl)ethylamino]-beta-elemene (IIm), and 13,14-bis(cyclohexamino)-beta-elemene (IIn) were the most potent agents. IIi, IIm, and IIn inhibited K562 cell growth with an IG50 below 5 microM that was correlated with mTOR activity inhibition.
Authors:
Liying Xu; Shujuan Tao; Xianming Wang; Zhiying Yu; Minwei Wang; Duo Chen; Yongkui Jing; Jinhua Dong
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2006-04-17
Journal Detail:
Title:  Bioorganic & medicinal chemistry     Volume:  14     ISSN:  0968-0896     ISO Abbreviation:  Bioorg. Med. Chem.     Publication Date:  2006 Aug 
Date Detail:
Created Date:  2006-06-20     Completed Date:  2006-09-22     Revised Date:  2009-11-19    
Medline Journal Info:
Nlm Unique ID:  9413298     Medline TA:  Bioorg Med Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  5351-6     Citation Subset:  IM    
Affiliation:
School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
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MeSH Terms
Descriptor/Qualifier:
Apoptosis / drug effects
Cell Line, Tumor
Cell Proliferation / drug effects
Cell Survival / drug effects
Drug Screening Assays, Antitumor
Hela Cells
Humans
Molecular Structure
Protein Kinases / drug effects*
Sesquiterpenes / chemical synthesis*,  chemistry,  pharmacology*
Stereoisomerism
Structure-Activity Relationship
Chemical
Reg. No./Substance:
0/Sesquiterpenes; 0/beta-elemene; EC 2.7.-/Protein Kinases; EC 2.7.1.-/mTOR protein

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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