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Molecules 2017, 22(7), 1087;

Synthesis and In Vitro Anticancer Activity of Novel Dehydroabietic Acid-Based Acylhydrazones

School of Chemistry and Chemical Engineering, Guangxi University, Nanning 530004, Guangxi, China
College of Pharmacy, Guilin Medical University, Guilin 541004, Guangxi, China
Author to whom correspondence should be addressed.
Received: 28 May 2017 / Revised: 24 June 2017 / Accepted: 26 June 2017 / Published: 29 June 2017
(This article belongs to the Section Medicinal Chemistry)
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In order to develop novel chemotherapeutic agents with potent anticancer activities, a series of dehydroabietic acid (DHA) derivatives bearing an acylhydrazone moiety were designed and synthesized by the condensation between dehydroabietic acylhydrazide (3) and a variety of substituted arylaldehydes. The inhibitory activities of these compounds against CNE-2 (nasopharynx), HepG2 (liver), HeLa (epithelial cervical), and BEL-7402 (liver) human carcinoma cell lines were evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay in vitro. The screening results revealed that many of the compounds showed moderate to high levels of anticancer activities against the tested cancer cell lines and some displayed similar potent inhibitory activities to the commercial anticancer drug cisplatin, while they exhibited lower cytotoxicity against normal human liver cell (HL-7702). Particularly, compound 4w, N’-(3,5-difluorobenzylidene)-2-(dehydroabietyloxy)acetohydrazide, with an IC50 (50% inhibitory concentration) value of 2.21 μM against HeLa cell, was about 17-fold more active than that of the parent compound, and showed remarkable cytotoxicity with an IC50 value of 14.46 μM against BEL-7402 cell. These results provide an encouraging framework that could lead to the development of potent novel anticancer agents. View Full-Text
Keywords: dehydroabietic acid; acylhydrazone; anticancer activity; synthesis dehydroabietic acid; acylhydrazone; anticancer activity; synthesis

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Li, F.-Y.; Wang, X.; Duan, W.-G.; Lin, G.-S. Synthesis and In Vitro Anticancer Activity of Novel Dehydroabietic Acid-Based Acylhydrazones. Molecules 2017, 22, 1087.

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