81467-89-2Relevant academic research and scientific papers
Synthesis and cell growth inhibitory properties of substituted (E)-1-phenylbut-1-en-3-ones
Ducki, Sylvie,Hadfield, John A.,Hepworth, Lucy A.,Lawrence, Nicholas J.,Ching-Ying, Liu,McGown, Alan T.
, p. 3091 - 3094 (1997)
A series of (E)-1-phenylbut-1-en-3-ones, based on the naturally occurring (E)-1-(4'-hydroxyphenyl)but-1-en-3-one [IC50 (K562) 60 μM], was synthesised and screened for cytotoxic activity against the K562 human leukaemia cell line. (E)-1-(Pentafluorophenyl)but-1-en-3-one [IC50 (K562) 1.8 μM] was found to be over 30-fold more active than 1.
9-norberberine derivative as well as preparation method and application thereof
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Paragraph 0039; 0046-0051, (2020/07/06)
The invention discloses a 9-norberberine derivative with antibacterial activity as well as a preparation method and application thereof. The invention provides a novel 9-norberberine derivative with antibacterial activity, and the berberine derivative has
Chiral δ-iodo-γ-lactones derived from cuminaldehyde, 2,5-dimethylbenzaldehyde and piperonal: Chemoenzymatic synthesis and antiproliferative activity
G?adkowski, Witold,Skrobiszewski, Andrzej,Mazur, Marcelina,Gliszczyńska, Anna,Czarnecka, Marta,Pawlak, Aleksandra,Obmińska-Mrukowicz, Bozena,Maciejewska, Gabriela,Bia?ońska, Agata
, p. 227 - 237 (2016/03/19)
Six enantiomeric pairs of β-aryl-δ-iodo-γ-lactones 8a-c, 9a-c derived from cuminaldehyde, 2,5-dimethylbenzaldehyde and piperonal were synthesized with high enantiomeric purities (ee 93-99%) from enantiomerically enriched allyl alcohols 3a-c. The key step
Design, synthesis and biological evaluation of novel C3-functionalized oxindoles as potential Pim-1 kinase inhibitors
Sun, Hong-Bao,Wang, Xiao-Yan,Li, Guo-Bo,Zhang, Li-Dan,Liu, Jie,Zhao, Li-Feng
, p. 29456 - 29466 (2015/04/14)
A novel series of C3-functionalized oxindoles, 3-(2-oxo-4-phenylbut-3-en-1-ylidene)indolin-2-ones, were designed, synthesized and investigated for inhibition of cell proliferation against different types of human cancer cell lines, including SW620, HeLa and A549. This biological study showed that these compounds containing the scaffolds of indole and aromatic α,β-unsaturated ketone had moderate to significant antitumor activities. Further study suggested that compound 4b, as one of this kind of structure derivative, showed broad-spectrum antitumor activities against MCF-7, PC-3, SKOV-3, U87, SMMC-7721, SY5Y and A875 cancer cell lines. Besides, the results of the inhibition of Pim kinases indicated that compound 4b showed selective and efficient anti-Pim-1 kinase activity (IC50 = 5 μM). Docking simulation, flow cytometry (FCM), and Hoechst 33342 staining assay suggested that the most active compound 4b induced cell death through apoptosis via binding to the active ATP pocket of Pim-1. Moreover, it showed that compound 4b had strong inhibition of tubulin polymerization which may be caused by inhibiting Pim-1. This journal is
Synthesis and anticancer activity of novel halolactones with β-aryl substituents from simple aromatic aldehydes
G?adkowski, Witold,Skrobiszewski, Andrzej,Mazur, Marcelina,Siepka, Monika,Pawlak, Aleksandra,Obmińska-Mrukowicz, Bozena,Bia?on?ska, Agata,Poradowski, Dominik,Drynda, Angelika,Urbaniak, Mariusz
, p. 10414 - 10423 (2013/11/19)
A series of 20 novel racemic iodo-, bromo- and chlorolactones, possessing β-phenyl-γ-lactone or β-phenyl-δ-lactone framework, were synthesized from commercially available aromatic aldehydes in convenient five-step syntheses. Some of them showed noticeable cytotoxic effect against two cancer lines, Jurkat (human leukaemia) and D17 (canine osteosarcoma). The highest activity, comparable with carboplatin, was observed for cis-5-(1-iodoethyl)-4-(4′-isopropylphenyl)dihydrofuran-2-one against Jurkat cell line.
