Design, Synthesis and Bioactivities of Novel 1,4-Pentadien-3-one Derivatives Containing a Substituted Pyrazolyl Moiety

In this study, in order to find novel biologically active penta-1,4-dien-3-one derivatives, a series of penta-1,4-dien-3-one compounds containing a substituted pyrazole subunit were designed and synthesized. Their structures were characterized by 1H-NMR, 13C-NMR and elemental analysis. The prelimina...

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Bibliographic Details
Main Authors: Cuili Chen, Jia Chen, Haiying Gu, Ning Bao, Hong Dai
Format: Article
Language:English
Published: MDPI AG 2017-07-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/22/7/1126
Description
Summary:In this study, in order to find novel biologically active penta-1,4-dien-3-one derivatives, a series of penta-1,4-dien-3-one compounds containing a substituted pyrazole subunit were designed and synthesized. Their structures were characterized by 1H-NMR, 13C-NMR and elemental analysis. The preliminary bioassays displayed that most of the title compounds showed significant antiproliferative activity against HepG2 cell lines. Especially, compounds 7a–m, o, r, s, u, w, y and z were active against HepG2 cells with IC50 values of 0.10–5.05 μM, which were superior to that of the contrast sorafenib (IC50 = 16.20 μM).
ISSN:1420-3049