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Linear diarylheptanoids as potential anticancer therapeutics: synthesis, biological evaluation, and structure-activity relationship studies

Title
Linear diarylheptanoids as potential anticancer therapeutics: synthesis, biological evaluation, and structure-activity relationship studies
Authors
Rahman, A. F. M. MotiurLu, YangLee, Hwa-JongJo, HyunjiYin, WencuiAlam, Mohammad SayedCha, HyochangKadi, Adnan A.Kwon, YoungjooJahng, Yurngdong
Ewha Authors
권영주
SCOPUS Author ID
권영주scopus
Issue Date
2018
Journal Title
ARCHIVES OF PHARMACAL RESEARCH
ISSN
0253-6269JCR Link

1976-3786JCR Link
Citation
ARCHIVES OF PHARMACAL RESEARCH vol. 41, no. 12, pp. 1131 - 1148
Keywords
Linear diarylheptanoidsTopoisomerase-ITopoisomerase-IIAntiproliferative activity
Publisher
PHARMACEUTICAL SOC KOREA
Indexed
SCIE; SCOPUS; KCI WOS
Document Type
Article
Abstract
In efforts to develop effective anticancer therapeutics with greater selectivity toward cancerous cell and reduced side-effects, such as emetic effects due to detrimental action of the drug toward the intestinal flora, a series of linear diarylheptanoids (LDHs) were designed and synthesized in 7 steps with good-to-moderate yields. All synthesized compounds were evaluated for their antibacterial, antiproliferative, and topoisomerase-I and -II inhibitory activity. Overall, all compounds showed little to no activity against the bacterial strains tested. Most of the synthesized compounds showed good antiproliferative activity against human breast cancer cell lines (T47D); specifically, the IC50 values of compounds 6a, 6d, 7j, and 7e were 0.09, 0.64, 0.67, and 0.99 M, respectively. Among the tested compounds, 7b inhibited topo-I by 9.3% (camptothecin 68.8%), 7e and 7h inhibited topo-II by 38.4 and 47.4% (etoposide 76.9%), respectively, at the concentration of 100M. These results suggest that a set of promising anticancer agents can be obtained by reducing inhibitory actions on different microbes to provide enhanced selectivity against cancerous cells.
DOI
10.1007/s12272-018-1004-8
Appears in Collections:
약학대학 > 약학과 > Journal papers
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