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 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).
Highlights
In the past few decades, curcumin, the principal curcuminoid of turmeric and its derivatives have attracted considerable attention due to their remarkable spectrum of biological activity, such as antimicrobial [1], anticancer [2], antioxidant [3], anti-inflammatory [4] and anti-HIV [5] activities.curcumin exhibits therapeutic promise for prostate cancer by interfering with cell proliferation through the induction of cell cycle arrest [6]
Despite that, accumulating evidence suggests that curcumin is highly unstable and has a poor bioavailability when tested in vitro and in vivo [8]
Many curcumin analogues have been studied for their activities by chemically modifying curcumin [9,10,11,12,13,14]
Summary
In the past few decades, curcumin, the principal curcuminoid of turmeric and its derivatives have attracted considerable attention due to their remarkable spectrum of biological activity, such as antimicrobial [1], anticancer [2], antioxidant [3], anti-inflammatory [4] and anti-HIV [5] activities.curcumin exhibits therapeutic promise for prostate cancer by interfering with cell proliferation through the induction of cell cycle arrest [6]. In the past few decades, curcumin, the principal curcuminoid of turmeric and its derivatives have attracted considerable attention due to their remarkable spectrum of biological activity, such as antimicrobial [1], anticancer [2], antioxidant [3], anti-inflammatory [4] and anti-HIV [5] activities. Curcumin is a potent anticancer agent with remarkable safety profile [7]. Despite that, accumulating evidence suggests that curcumin is highly unstable and has a poor bioavailability when tested in vitro and in vivo [8]. This has triggered extensive research in search for curcumin analogues and mimics with improved potency and pharmacokinetic profiles for the potential clinical treatment of cancers.
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