Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 86, Issue -, Pages 684-689Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.09.026
Keywords
Annonaceous acetogenin; Antitumor activity; Chemical synthesis; Structure-activity relationship
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Funding
- Ministry of Education, Culture, Sports, Science and Technology, Japan (MEXT)
- Japan Society for the Promotion of Sciences (JSPS) [21790113, 23790130, 25460159, 22390021]
- MEXT-Supported Program for the Strategic Research Foundation at Private Universities [S0801063]
- Grants-in-Aid for Scientific Research [25460159, 21790113, 22390021] Funding Source: KAKEN
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Five novel acetogenin analogues with a furan, thiophene, or thiazole ring were synthesized, and their inhibitory activities toward human cancer cell lines were evaluated. The analogues showed more potent activities than natural acetogenin. One of them, the thiophene-3-carboxamide analogue, strongly inhibited the growth of human lung cancer cell line NCI-H23 in the xenograft mouse assay without critical toxicity. (C) 2014 Elsevier Masson SAS. All rights reserved.
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