23066-93-5Relevant academic research and scientific papers
Simple 2(5H)-furanone derivatives with selective cytotoxicity towards non-small cell lung cancer cell line A549 – Synthesis, structure-activity relationship and biological evaluation
Byczek-Wyrostek, Anna,Kitel, Radoslaw,Rumak, Klaudia,Skonieczna, Magdalena,Kasprzycka, Anna,Walczak, Krzysztof
, p. 687 - 697 (2018)
A series of 5-alkoxy derivatives of 3,4-dichloro-5-hydroxyfuran-2-(5H)-one (mucochloric acid, MCA) were obtained and subsequently subjected to modification in the C-4 position of 2(5H)-furanone ring. The cytotoxicity of newly synthesized compounds was evaluated in MTT assay against non-small cell lung cancer (A549) and healthy lung epithelial cell line (BEAS-2B). The derivatives containing a branched alkoxy substituent in the C-5 position demonstrated the highest anticancer properties, whereas modification of compounds in the C-4 position of 2(5H)-furanone ring only slightly improve their antiproliferative properties. Compounds 12 and 15 exhibited the best selectivity towards A549 cells and were also evaluated in a panel of cancer cell lines of different origin. Further investigation revealed that treatment of A549 cell line with compounds 12 and 15 led to G2 phase cell cycle arrest and induction of caspase-independent cell death. Moreover, compound 12 was found to act synergistically with erlotinib.
Synthesis of artemisinin-piperazine-furan ether hybrids and evaluation of in vitro cytotoxic activity
Wei, Meng-Xue,Yu, Jia-Ying,Liu, Xin-Xin,Li, Xue-Qiang,Zhang, Meng-Wei,Yang, Pei-Wen,Yang, Jin-Hui
, (2021)
For the first time, eight novel artemisinin-piperazine-furane ether hybrids (5a?h) were efficiently synthesized and investigated for their in vitro cytotoxic activity against some human cancer and benign cells. The absolute configuration of hybrid 5c was
Synthesis and biological evaluation of novel artemisone-piperazine-tetronamide hybrids
He, Yu,Li, Xue-Qiang,Liu, Xin-Xin,Wei, Meng-Xue,Yang, Jin-Hui,Yang, Pei-Wen,Yu, Jia-Ying,Zhang, Meng-Wei,Zhang, Si-Si
, p. 18333 - 18341 (2021/05/31)
For the first time, six novel artemisone-piperazine-tetronamide hybrids (12a-f) were efficiently synthesised from dihydroartemisinin (DHA) and investigated for their in vitro cytotoxicity against some human cancer cells and benign cells. All the targets s
Preparation and use of halobutenolide-like compound having insecticidal activity
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Paragraph 0032; 0033; 0034, (2019/02/25)
The invention discloses preparation and use of a halobutenolide-like compound having insecticidal activity. The invention relates to a nitrogen-containing ring-opening compound having a formula (A) where R1, R2, R3 and X are each as defined in the specification. The invention discloses a preparation method of a novel insecticide and the use thereof. The compound and a derivative thereof are used for agricultural and forestry pests with high insecticidal activity such as homoptera and lepidoptera: aphids, planthoppers, whiteflies, leafhoppers, thrips, cotton bollworm, cabbage caterpillar, plutella xylostella, prodenia litura, and armyworm.
Synthesis of amino acid derivatives of 5-alkoxy-3,4-dihalo-2(5: H)-furanones and their preliminary bioactivity investigation as linkers
Luo, Shi-He,Yang, Kai,Lin, Jian-Yun,Gao, Juan-Juan,Wu, Xin-Yan,Wang, Zhao-Yang
, p. 5138 - 5147 (2019/05/29)
A series of amino acid derivatives are successfully synthesized via a metal-free C-N coupling reaction of 5-alkoxy-3,4-dihalo-2(5H)-furanones and amino acids. Their structures are well characterized with 1H NMR, 13C NMR, ESI-MS and elemental analysis. As potential linkers of the 2(5H)-furanone unit with other drug moieties containing a hydroxyl or amino group, the effect of amino acids is investigated by comparison with other 2(5H)-furanone compounds by constructing C-O/C-S bonds. The preliminary results of the biological activity assay by the MTT method on a series of cancer cell lines in vitro reveal that the introduction of amino acids basically has no toxic effect. This can lead to these 2(5H)-furanone derivatives being further well-linked with other bioactive moieties with amino or hydroxy groups as expected. Thus, the biological activity assay gives a direction for the design of bioactive 2(5H)-furanones based on these amino acid linkers.
COMPOSITIONS AND METHODS FOR VIRAL SENSITIZATION
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Paragraph 0048; sheet 3, (2016/08/23)
Provided are compounds that enhance the efficacy of viruses by increasing spread of the virus in cells, increasing the titer of virus in cells, or increasing the antigen expression from a virus, gene or trans-gene expression from a virus, or virus protein expression in cells. Other uses, compositions and methods of using same are also provided.
3,4-dihalo-2(5H)-furanones: A novel oxidant for the Glaser coupling reaction
Li, Jian-Xiao,Liang, Hao-Ran,Wang, Zhao-Yang,Fu, Jian-Hua
scheme or table, p. 507 - 513 (2011/12/16)
5-Alkoxy-3,4-dihalo-2(5H)-furanones could be used as a kind of novel oxidant in the Glaser coupling reaction. The screening of reaction conditions showed that both PdCl2(PPh3)2 and 3,4-dichloro-5-methoxy-2(5H)-furanone played crucial roles in the reaction. A possible reaction mechanism was proposed according to the reactivity of 3,4-dihalo-2(5H)-furanones. The new method easily allows the syntheses of alkyl and aryl substituted 1,3-diyne compounds. However, carbyne polymer was unexpectedly obtained when using trimethylsilyl acetylene as the substrate under the Glaser reaction condition.
NOVEL 4-AMINO-2(5H)-FURANONES
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Page 21-22, (2008/06/13)
The present invention relates to compounds of formula (I): wherein X is selected from hydrogen, a halogen, a substituted or unsubstituted cyclic and heterocyclic moiety, substituted or unsubstituted, linear or branched alkyl, alkyloxy, alkylcarbonyl, alky
