65623-98-5Relevant academic research and scientific papers
Folic acid-conjugated europium complexes as luminescent probes for selective targeting of cancer cells
Quici, Silvio,Casoni, Alessandro,Foschi, Francesca,Armelao, Lidia,Bottaro, Gregorio,Seraglia, Roberta,Bolzati, Cristina,Salvarese, Nicola,Carpanese, Debora,Rosato, Antonio
, p. 2003 - 2014 (2015)
We report the synthesis of three optical probes (Eu3+1, Eu3+2, and Eu3+3) having a luminescent Eu complex (signaling unit) bonded in different positions to folic acid (FA), the folate receptor (FR) targeting unit. The structures of the two regioisomers Eu3+1 and Eu3+2 were assigned by mass spectrometric experiments. The optical properties and stability of these probes were assessed in phosphate-buffered saline, cell culture medium, rat serum, and cellular lysate, and results indicated that they are chemically and photophysically stable. Cytotoxicity was studied with ovarian cancer cells having high (SKOV-3), intermediate (OVCAR-3), low (IGROV-1), or null (A2780) expression of FRs. The internalized probe, evaluated in SKOV-3, IGROV-1, and A2780 cells, was in the order Eu3+2 > Eu3+1 > Eu3+3. No internalization was observed for A2780 cells. Such results, together with those obtained in competition experiments of FA versus Eu3+2 and FA or Eu3+2 versus 3H-FA, indicate that internalization is receptor-mediated and that Eu3+2 shows high selectivity and specificity for FR.
PH-Gated photoresponsive shuttling in a water-soluble pseudorotaxane
Zubillaga,Ferreira,Parola,Gago,Basílio
, p. 2743 - 2746 (2018)
A fluorescent bistable pseudorotaxane was devised and shown to display pH-gated photoresponsive ring shuttling. At pH > 7.5 shuttling does not take place after light stimulation while at pH ≈ 5 the macrocycle is quantitatively translocated.
NOVEL COMPOUND FOR ORGANIC LIGHT EMITTING DIODE AND COATING COMPOSITION FOR ORGANIC LAYER COMPRISING THE SAME
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Paragraph 0304-0306, (2021/08/31)
Provided are a compound represented by chemical formula (1) and a coating liquid composition comprising the same. The above formula (1) is as described in the description of the invention.
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
CLASS OF BIFUNCTIONAL COMPOUNDS WITH QUATERNARY AMMONIUM SALT STRUCTURE
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Paragraph 0249, (2019/11/11)
The invention provides a class of compounds represented by formula (I), having bifunctional active quaternary ammonium salt structure of a β2-adrenoreceptor agonist and an M receptor antagonist, a pharmaceutically acceptable salt, solvate, and optical isomer thereof. A pharmaceutical composition comprising such a compound with quaternary ammonium salt structure, a method for preparing such a compound with quaternary ammonium salt structure and an intermediate thereof, and uses thereof in treating pulmonary disorders are also provided. The compounds of the invention have high selectivity to the M receptor subtype, and have less adverse reaction and lower toxic and side effects in the treatment of pulmonary diseases such as COPD and asthma.
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
Optimization and preclinical evaluation of novel histamine H3 receptor ligands: Acetyl and propionyl phenoxyalkyl piperazine derivatives
Szczepańska, Katarzyna,Karcz, Tadeusz,Kotańska, Magdalena,Siwek, Agata,Kuder, Kamil J.,Latacz, Gniewomir,Mogilski, Szczepan,Hagenow, Stefanie,Lubelska, Annamaria,Sobolewski, Micha?,Stark, Holger,Kie?-Kononowicz, Katarzyna
supporting information, p. 6056 - 6066 (2018/11/23)
As a continuation of our search for novel histamine H3 receptor ligands, a series of new acetyl and propionyl phenoxyalkylamine derivatives (2–25) was synthesized. Compounds with three to four carbon atoms alkyl chain spacer, composed of six various 4N-substituted piperazine moieties were evaluated for their binding properties at human histamine H3 receptors (hH3R). In vitro test results proved the 4-pyridylpiperazine moiety as crucial element for high hH3R affinity (hH3R Ki = 5.2–115 nM). Moreover introduction of carbonyl group containing residues in the lipophilic part of molecules instead of branched alkyl substituents resulted in increased affinity in correlation to previously described series, whereas propionyl derivatives showed slightly higher affinities than those of acetyl (16 and 22 vs. 4 and 10; hH3R Ki = 5.2 and 15.4 nM vs. 10.2 and 115 nM, respectively). These findings were confirmed by molecular modelling studies, demonstrating multiple ligand-receptor interactions. Furthermore, pharmacological in vivo test results of compound 4 clearly indicate that it may affect the amount of calories consumed, thus act as an anorectic compound. Likewise, its protective action against hyperglycemia and the development of overweight has been shown. In order to estimate drug-likeness of compound 4, in silico and experimental evaluation of metabolic stability in human liver microsomes was performed.
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 0109; 0110, (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
