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Molecules 2017, 22(7), 1126; doi:10.3390/molecules22071126

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

1,2
,
3
,
1,2,* , 2
and
3,*
1
College of Chemistry, Chemical Engineering and Materials Science, Soochow University, Suzhou 215123, China
2
School of Public Health, Nantong University, Nantong 226019, China
3
College of Chemistry and Chemical Engineering, Nantong University, Nantong 226019, China
*
Authors to whom correspondence should be addressed.
Received: 26 May 2017 / Revised: 28 June 2017 / Accepted: 5 July 2017 / Published: 6 July 2017
(This article belongs to the Section Organic Synthesis)
View Full-Text   |   Download PDF [895 KB, uploaded 6 July 2017]   |  

Abstract

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 7am, 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). View Full-Text
Keywords: penta-1,4-dien-3-one; pyrazole; synthesis; biological activity penta-1,4-dien-3-one; pyrazole; synthesis; biological activity
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    Description: 1H NMR and 13C NMR spectra of pyrazole oxime compounds 7a-7z

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Chen, C.; Chen, J.; Gu, H.; Bao, N.; Dai, H. Design, Synthesis and Bioactivities of Novel 1,4-Pentadien-3-one Derivatives Containing a Substituted Pyrazolyl Moiety. Molecules 2017, 22, 1126.

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