Document Detail

Design, synthesis and in vitro evaluation of novel dehydroabietic acid derivatives containing a dipeptide moiety as potential anticancer agents.
MedLine Citation:
PMID:  25462253     Owner:  NLM     Status:  Publisher    
A series of novel dehydroabietic acid (DHA) chiral dipeptide derivatives were designed and synthesized as potent antitumor agents. The inhibitory activities of these compounds against NCI-H460 (lung), HeLa (epithelial cervical) and MGC-803 (gastric) human cancer cell lines were estimated by MTT assay in vitro. The antitumor activities screening indicated that many compounds showed moderate to high levels of antitumor activities against these three cancer cell lines and most of these compounds displayed more potent inhibitory activities compared with commercial anticancer drug 5-fluorouracil (5-FU). The induction of apoptosis and affects on the cell cycle distribution with compound 8k were investigated by acridine orange/ethidium bromide staining, Hoechst 33258 staining, JC-1 mitochondrial membrane potential staining, TUNEL assay, flow cytometry and the activities of caspase-3 and -9 assay in Hela cells, which exhibited that the compound could induce cell apoptosis in Hela cells. In addition, further investigation showed that apoptosis were associated with loss of mitochondrial membrane potential, enhancement of mitochondrial cytochrome c release and intracellular ROS production, elevation of Bax expression, down-regulation of Bcl-2, and the activation of caspase-9 and -3.
Xiao-Chao Huang; Le Jin; Meng Wang; Dong Liang; Zhen-Feng Chen; Ye Zhang; Ying-Ming Pan; Heng-Shan Wang
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2014-10-22
Journal Detail:
Title:  European journal of medicinal chemistry     Volume:  89C     ISSN:  1768-3254     ISO Abbreviation:  Eur J Med Chem     Publication Date:  2014 Oct 
Date Detail:
Created Date:  2014-12-2     Completed Date:  -     Revised Date:  2014-12-3    
Medline Journal Info:
Nlm Unique ID:  0420510     Medline TA:  Eur J Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  370-385     Citation Subset:  -    
Copyright Information:
Copyright © 2014 Elsevier Masson SAS. All rights reserved.
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