55368-24-6Relevant academic research and scientific papers
Design, synthesis, and anti-proliferative evaluation of 1: H -1,2,3-triazole grafted tetrahydro-β-carboline-chalcone/ferrocenylchalcone conjugates in estrogen responsive and triple negative breast cancer cells
Awolade, Paul,Cele, Nosipho,Gu, Liang,Kaur, Mandeep,Kumar, Vipan,Pillay, Ruvesh Pascal,Sharma, Bharvi,Singh, Parvesh
, p. 11137 - 11147 (2020/07/15)
A series of 1H-1,2,3 triazole grafted tetrahydro-β-carboline-chalcone/ferrocenylchalcone conjugates were synthesized and in vitro evaluated against estrogen responsive (MCF-7) and triple negative (MDA-MB-231) breast cancer cells. Comparative analysis reve
New rosiglitazone analogue, preparation method and applications thereof
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Paragraph 0159-0163, (2020/01/12)
The invention relates to a rosiglitazone analogue, a preparation method and applications thereof, wherein the compound has a structure represented by the following formula (I), R1 represents C3-10 cycloalkyl unsubstituted or optionally substituted by the
Structural modifications and in vitro pharmacological evaluation of 4-pyridyl-piperazine derivatives as an active and selective histamine H3 receptor ligands
Szczepańska, Katarzyna,Karcz, Tadeusz,Siwek,Kuder, Kamil J.,Latacz, Gniewomir,Bednarski,Szafarz, Ma?gorzata,Hagenow, Stefanie,Lubelska, Annamaria,Olejarz-Maciej, Agnieszka,Sobolewski, Micha?,Mika,Kotańska, Magdalena,Stark, Holger,Kie?-Kononowicz, Katarzyna
supporting information, (2019/07/31)
A novel series of 4-pyridylpiperazine derivatives with varying alkyl linker length and eastern part substituents proved to be potent histamine H3 receptor (hH3R) ligands in the nanomolar concentration range. While paying attention to
Synthesis of new chalcone-based homoserine lactones and their antiproliferative activity evaluation
Yu, Bin,Liu, Haoyue,Kong, Xiaoyan,Chen, Xinli,Wu, Chunli
, p. 500 - 511 (2019/01/03)
Three series of new homoserine lactone analogs were efficiently synthesized starting from methionine and further evaluated for their antiproliferative activity against different cancer cell lines. Among these compounds, some of the chalcone containing compounds 6a-n showed acceptable antiproliferative activity against prostate cancer cells DU145 and PC-3 with the IC50 values less than 10 μM. Compounds 6c, 6e and 6h inhibited growth of DU145 and PC-3 cells at low micromolar levels with the IC50 values ranging from 3.0 to 5.0 μM, much more potent than natural OdDHL. Compound 6e concentration-dependently inhibited colony formation and cell migration of DU145 cells. A synergistic effect on the growth inhibition and the apoptosis of DU145 cells was observed when compound 6e was used in combination with TRAIL. OdDHL or 6e treatment concentration-dependently activated TRAIL death receptor DR5 which may account for the observed synergistic effect of 6e or OdDHL with TRAIL on the growth inhibition and cell apoptosis. Compound 6e also inhibited migration of DU145 cells in a time- and concentration-dependent manner. The data suggest that quorum sensing molecules OdDHL and 6e may improve the sensitivity of DU145 cells toward TRAIL via activating DR5, compound 6e may be used as a potential lead compound for developing new TRAIL receptor agonists.
Adenine derivatives invert high glucose-induced thioredoxin-interacting protein overexpression
Zhong, Li,Liu, Qing,Ting, Yan Sie,Thien, Vun Yien,Binti Kalong, Nurwafa Syafiqah,Yang, Dehua,Wang, Ming-Wei
, p. 1998 - 2008 (2018/09/21)
Overexpression of thioredoxin-interacting protein (TXNIP) is associated with reduced insulin sensitivity and β-cell apoptosis. We have previously shown that W2476 inhibited high glucose-induced TXNIP expression at both mRNA and protein levels in INS-1E ce
W2476 ameliorates β-cell dysfunction and exerts therapeutic effects in mouse models of diabetes via modulation of the thioredoxin-interacting protein signaling pathway
Li, Ting,Lin, Guang-Yao,Zhong, Li,Zhou, Yan,Wang, Jia,Zhu, Yue,Feng, Yang,Cai, Xiao-Qing,Liu, Qing,Nosjean, Olivier,Boutin, Jean A,Renard, Pierre,Yang, De-Hua,Wang, Ming-Wei
, p. 1024 - 1037 (2017/07/11)
Recent evidence shows that high glucose levels recruit carbohydrate response element-binding protein, which binds the promoter of thioredoxin-interacting protein (txnip), thereby regulating its expression in β-cells. Overexpression of txnip not only induc
4-Aminoquinoline-ferrocenyl-chalcone conjugates: Synthesis and anti-plasmodial evaluation
Singh, Amandeep,Gut, Jiri,Rosenthal, Philip J.,Kumar, Vipan
, p. 269 - 277 (2016/10/03)
A series of aliphatic and aromatic substituted 1H-1,2,3-triazole-tethered 4-amino-quinoline-ferrocenylchalcone conjugates has been synthesized and evaluated for anti-plasmodial activity. The conjugates with flexible aliphatic (aminoethanol or aminopropano
Piperazine-linked 4-aminoquinoline-chalcone/ferrocenyl-chalcone conjugates: Synthesis and antiplasmodial evaluation
Singh, Amandeep,Rani, Anu,Gut, Jiri,Rosenthal, Philip J.,Kumar, Vipan
, p. 590 - 595 (2017/09/14)
A series of piperazine-linked 4-aminoquinoline-chalcone/ferrocenyl-chalcone conjugates were prepared with a view to evaluate their activities against Plasmodium falciparum. The synthesized conjugates had in vitro IC50 values from 0.41 to 2.38?μ
Farnesyl thioether substituted chalcone derivatives and its preparation and use
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Paragraph 0106; 0107, (2016/10/08)
The invention discloses a farnesylated thioether-substituted chalcone derivative, a preparation method and a purpose thereof. The invention relates to the farnesylated thioether-substituted chalcone derivative shown in a general formula (I), (II) and (III
DOPAMINE D2 RECEPTOR LIGANDS
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Page/Page column 125; 126, (2016/07/05)
The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopaminergic activity. The present invention relates to novel compounds that modulate dopamine D2 receptors. In particular, compounds of the present invention show functional selectivity at the dopamine D2 receptors and exhibit selectivity downstream of the D2 receptors, on the 0- arrestin pathway and/or on the cAMP pathway.
