期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 143, 期 -, 页码 948-957出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2017.10.079
关键词
Triterpene acid; Myrrhanone B; Antiproliferation; Docking study
资金
- Oman Research Council (TRC) [ORG/HSS/14/004]
- Science Campus Halle WCH [W13004216]
In the current investigation, new monomers of myrrhanone B and lupeolic acid were prepared via reaction of triterpenic acids with linkers in the presence of K2CO3. In addition, new bis-myrrhanone B homodimers, myrrhanone B-myrrhanol B heterodimers, and bis-myrrhanone beta-boswellic acids heterodimer were prepared. Evaluation of these compounds on the proliferation of four different human cancer cell lines, viz., FaDu (pharynx carcinoma), A2780 (ovarian carcinoma), HT29 (colon adenocarcinoma) and A375 (malignant melanoma) has been performed. It is worth mentioning that compounds 4, 7, 8,10, and 11 possess potent antiproliferative effect towards HT29 cancer cells with IC50 values of 8.1 mu M, 5.4 mu M, 8.8 1 mu M, 6.8 mu M, and 8.2 mu M, respectively. In addition, these compounds display good to moderate antiproliferative activities towards A2780 and A375 with IC50 values ranging from 10.4 to 24.2 mu M. Moreover, the molecular docking studies of most active compounds (4, 7, 8, 10 and 11) with six anticancer drug targets DHFR, VEGFR2, HER-2/neu, CDK6, hCA-IX and LOX also carried, in order to know the mode of binding interaction and energy of this class of compounds. (C) 2017 Elsevier Masson SAS. All rights reserved.
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