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

被引：5

作者：

Chen, Cuili ^{[1
,2
]}

Chen, Jia ^{[3
]}

Gu, Haiying ^{[1
,2
]}

Bao, Ning ^{[2
]}

Dai, Hong ^{[3
]}

机构：

[1] Soochow Univ, Coll Chem Chem Engn & Mat Sci, Suzhou 215123, Peoples R China

[2] Nantong Univ, Sch Publ Hlth, Nantong 226019, Peoples R China

[3] Nantong Univ, Coll Chem & Chem Engn, Nantong 226019, Peoples R China

来源：

MOLECULES | 2017年 / 22卷 / 07期

基金：

中国国家自然科学基金;

关键词：

penta-1,4-dien-3-one; pyrazole; synthesis; biological activity; BIOLOGICAL EVALUATION; CURCUMIN; ANALOGS; AGENTS; KINETICS; GROWTH;

D O I：

10.3390/molecules22071126

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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 H-1-NMR, C-13-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 mu M, which were superior to that of the contrast sorafenib (IC50 = 16.20 mu M).

引用

页数：12

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