99733-18-3Relevant academic research and scientific papers
Molecular recognition in bisurea thermoplastic elastomers studied with pyrene-based fluorescent probes and atomic force microscopy
Botterhuis, Nicole E.,Karthikeyan,Veldman, Dirk,Meskers, Stefan C. J.,Sijbesma, Rint P.
, p. 3915 - 3917 (2008)
Fluorescence spectroscopy and atomic force microscopy (AFM) measurements using bisurea-pyrene probes show that they are randomly dispersed in the hard blocks of thermoplastic elastomers with matching bisurea groups, whereas they phase separate from polymers with non-matching or no bisurea groups. The Royal Society of Chemistry.
HMG-COA REDUCTASE DEGRADATION INDUCING COMPOUND
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Paragraph 893-896, (2021/10/11)
The present invention relates HMG-CoA reductase degradation inducing compounds. Specifically, the present invention relates a bifunctional compound in which a HMG-CoA reductase binding moiety and an E3 ubiquitin ligase-binding moiety are linked by a chemical linker. The present invention also relates a method for preparing the compounds, and a method for degradation of HMG-CoA reducatase using the compounds, as well as use for prevention or treatment of HMG-CoA reductase related diseases using the compounds.
Design, synthesis and biological evaluation of tyrosinase-targeting PROTACs
Cui, Xin,Deng, Yun,Fu, Dingqiang,Li, Guangxun,Qin, Fengming,Tang, Zhuo,Xu, Yan,Yao, Shaohua,Yuan, Yi
supporting information, (2021/10/12)
The human tyrosinase is the most prominent therapeutic target for pigmentary skin disorders. However, the overwhelming majority efforts have been devoted to search mushroom tyrosinase inhibitors, which show poor inhibitory activity on human tyrosinase and certain side effects that cause skin damage in practical application. Herein, a series of degraders that directly targeted human tyrosinase was firstly designed and synthesized based on newly developed PROTAC technology. The best PROTAC TD9 induced human tyrosinase degradation obviously in dose and time-dependent manner, and its mechanism of inducing tyrosinase degradation has also been clearly demonstrated. Besides, encouraging results that low-toxicity PROTAC TD9 was applied to reduce zebrafish melanin synthesis have been obtained, highlighting the potential to treatment of tyrosinase-related disorders. Moreover, this work has innovatively expanded the application scope of PROTAC technology and laid a solid foundation for further development of novel drugs treating pigmentary skin disorders.
JNK Inhibitor. Pharmaceutical compositions and uses thereof
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Paragraph 0130-0133, (2021/11/27)
Provided herein are compounds represented by the following formula (I), racemates, stereoisomers, tautomers, isotopically labels, solvates, polymorphs, nitrogen oxides or pharmaceutically acceptable salts thereof, which can be used as JNK inhibitors. A method for preparing a compound represented by formula (I), a pharmaceutical composition comprising a compound represented by formula (I), and (I), for the preparation of a medicament for the treatment of a disease treatable by inhibition JNK activity.
Fluorescent H2Receptor Squaramide-Type Antagonists: Synthesis, Characterization, and Applications
Alencastre, Inês,Bernhardt, Günther,Biselli, Sabrina,Buschauer, Armin,Chen, Mengya,Erdmann, Daniela,Gomez-Lazaro, Maria,Keller, Max,Lamghari, Meriem,Littmann, Timo,Maia, André F.,Ozawa, Takeaki,Tanaka, Miho,Tropmann, Katharina
supporting information, p. 1521 - 1528 (2020/09/15)
Fluorescence labeled ligands have been gaining importance as molecular tools, enabling receptor-ligand-binding studies by various fluorescence-based techniques. Aiming at red-emitting fluorescent ligands for the hH2R, a series of squaramides labeled with pyridinium or cyanine fluorophores (19-27) was synthesized and characterized. The highest hH2R affinities in radioligand competition binding assays were obtained in the case of pyridinium labeled antagonists 19-21 (pKi: 7.71-7.76) and cyanine labeled antagonists 23 and 25 (pKi: 7.67, 7.11). These fluorescent ligands proved to be useful tools for binding studies (saturation and competition binding as well as kinetic experiments), using confocal microscopy, flow cytometry, and high content imaging. Saturation binding experiments revealed pKd values comparable to the pKi values. The fluorescent probes 21, 23, and 25 could be used to localize H2 receptors in HEK cells and to determine the binding affinities of unlabeled compounds.
COMPOUNDS AND METHODS FOR MODULATING RNA FUNCTION
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Paragraph 00444; 00445, (2018/02/28)
The present invention provides compounds, compositions thereof, and methods of using the same.
COMPOUNDS AND METHODS OF TREATING RNA-MEDIATED DISEASES
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Paragraph 00384; 00385, (2017/12/27)
The present invention provides compounds, compositions thereof, and methods of using the same.
Synthesis and biological evaluation of the first dual tyrosyl-DNA phosphodiesterase i (Tdp1)-topoisomerase i (Top1) inhibitors
Nguyen, Trung Xuan,Morrell, Andrew,Conda-Sheridan, Martin,Marchand, Christophe,Agama, Keli,Bermingam, Alun,Stephen, Andrew G.,Chergui, Adel,Naumova, Alena,Fisher, Robert,O'Keefe, Barry R.,Pommier, Yves,Cushman, Mark
scheme or table, p. 4457 - 4478 (2012/08/07)
Substances with dual tyrosyl-DNA phosphodiesterase I-topoisomerase I inhibitory activity in one low molecular weight compound would constitute a unique class of anticancer agents that could potentially have significant advantages over drugs that work against the individual enzymes. The present study demonstrates the successful synthesis and evaluation of the first dual Top1-Tdp1 inhibitors, which are based on the indenoisoquinoline chemotype. One bis(indenoisoquinoline) had significant activity against human Tdp1 (IC 50 = 1.52 ± 0.05 μM), and it was also equipotent to camptothecin as a Top1 inhibitor. Significant insights into enzyme-drug interactions were gained via structure-activity relationship studies of the series. The present results also document the failure of the previously reported sulfonyl ester pharmacophore to confer Tdp1 inhibition in this indenoisoquinoline class of inhibitors even though it was demonstrated to work well for the steroid NSC 88915 (7). The current study will facilitate future efforts to optimize dual Top1-Tdp1 inhibitors.
Self-sorting of guests and hard blocks in bisurea-based thermoplastic elastomers
Botterhuis, Nicole E.,Karthikeyan,Spiering,Sijbesma, Rint P.
scheme or table, p. 745 - 751 (2011/10/02)
Self-sorting in thermoplastic elastomers was studied using bisurea-based thermoplastic elastomers (TPEs) which are known to form hard blocks via hierarchical aggregation of bisurea segments into ribbons and of ribbons into fibers. Self-sorting of different bisurea hard blocks in mixtures of polymers to give separate ribbons was established by studying exciplex formation between fluorescent pyrene and dimethylaniline (DMA) functionalized bisurea probes. If both probes had the same spacing between the bisurea units as the matrix hard segments, exciplex bands were observed in the fluorescence emission spectra, whereas exciplex intensities were strongly reduced when DMA and pyrene probes with, different spacer lengths were incorporated in a mixed matrix that provided matching host segments for each guest separately. Probes with butylene spaced bisurea groups showed the highest degree of self-sorting. Self-sorting was further improved by annealing of the polymer films leading to a degree of self-sorting of more than 95%. Self-sorting at the fiber level of aggregation was studied by fluorescence resonance energy transfer (FRET) between naphthalene (donor) and pyrene (acceptor) bisurea guests. Large differences in FRET behavior for matching and nonmatching probes showed that significant self-sorting takes places between ribbons to give separate fibers.
OXOBENZINDOLIZINOQUINOLINES AND USES THEREOF
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Page/Page column 42, (2009/12/23)
The synthesis of aromathecins, substituted 12H-5,l la-diazadibenzo[b,h]fluoren- 11 -ones is described. Use of these cytotoxic compounds and pharmaceutical compositions containing them for the treatment of cancer is described. Two novel processes for the synthesis of this system and a series of 14-substituted aromathecins as novel cytotoxic, topoisomerase I poisons are described.
