7530-31-6Relevant articles and documents
Discriminating detection of multiple analytes (F- and CN-) by a single probe through colorimetric and fluorescent dual channels
Wang, Ying,Zhao, Qian,Zang, Libin,Liang, Chunshuang,Jiang, Shimei
, p. 166 - 175 (2015)
Abstract Two novel Schiff base type receptors containing phenol hydroxyl group (1) or methoxy group (2) were designed and synthesized. The receptor 1 with phenol hydroxyl group exhibited different colorimetric and fluorimetric responses to fluoride and cy
Interior Surface Modification of Bacteriophage MS2
Hooker, Jacob M.,Kovacs, Ernest W.,Francis, Matthew B.
, p. 3718 - 3719 (2004)
An efficient strategy for the interior surface functionalization of MS2 viral capsids is reported, featuring a new hetero-Diels?Alder bioconjugation reaction. After virus isolation, the RNA genome was removed from the spherical particles by exposure to pH 11.8 conditions for a period of 4 h. Following this, 180 tyrosine residues on the interior surface of each empty capsid shell were modified by using a site-selective diazonium-coupling reaction. To attach additional functionality, the azo conjugate was reduced with Na2S2O4 to afford an ortho-amino tyrosine derivative. Oxidation of this moiety with NaIO4 produced an o-iminoquinone on the protein surface, which was found to undergo an efficient hetero-Diels?Alder reaction with N-(4-aminophenyl)acrylamide. This four-step procedure can be carried out in under 4 h, reaches high levels of conversion, and yields the desired conjugates in >60% overall yield. Copyright
Design, synthesis and structure-activity relationship of diaryl-ureas with novel isoxazol[3,4-b]pyridine-3-amino-structure as multi-target inhibitors against receptor tyrosine kinase
Shi, Zhi-Hao,Liu, Feng-Tao,Tian, Hao-Zhong,Zhang, Yan-Min,Li, Nian-Guang,Lu, Tao
, p. 4735 - 4744 (2018/08/21)
Inspired by that the multi-target inhibitors against receptor tyrosine kinases (RTKs) have significantly improved the effect of clinical treatment for cancer, and based on the chemical structure of Linifanib (ABT-869, Abbott), two series of diaryl-ureas with novel isoxazol[3,4-b]pyridine-3-amino-structure were designed and synthesized as multi-target inhibitors against RTKs. The preliminary biological evaluation showed that several compounds exhibited comparable potency with Linifanib. Compound S21 was identified as the most potent inhibitor against Fms-like tyrosine kinase 3 (FLT-3), kinase insert domain containing receptor (KDR) and platelet-derived growth factor receptor β (PDGFR-β) with its IC50 values were 4 nM, 3 nM and 8 nM respectively, it also showed potent inhibitory activities against several cancer cells.
PYRAZOLOPYRIMIDINE DERIVATIVES, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION FOR USE IN PREVENTING OR TREATING CANCER, AUTOIMMUNE DISEASE AND BRAIN DISEASE CONTAINING THE SAME AS AN ACTIVE INGREDIENT
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, (2018/12/02)
The present invention relates to a pyrazolopyrimidine derivative, a preparation method thereof and a pharmaceutical composition comprising the same as an active ingredient for the prevention or treatment of cancer, autoimmune disease and brain disease. The pyrazolopyrimidine derivative of the present invention exhibits excellent Bruton's tyrosine kinase inhibition activity, so that it can be effectively used as a pharmaceutical composition for the prevention or treatment of cancer, autoimmune disease and Parkinson's disease.
A polymerizable monomer preparation method and application of
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Paragraph 0053; 0055; 0056; 0057; 0071; 0072; 0083; 0084, (2017/08/25)
The invention provides a preparation method and application of a polymerizable monomer. The method comprises the following steps of: (1) under the condition of an amidation reaction, enabling aromatic diamine with the structure as shown in the formula (I) to be in contact with acrylic so as to obtain an intermediate M with the structure as shown in the formula (II); and (2)under the condition of a condensation reaction, enabling the intermediate M to be in contact with binary fatty acid with the structure as shown in the formula (III) so as to obtain the polymerizable monomer as shown in the formula (IV), wherein n is an integer of 0-5, and m is an integer of 1-10. The purity and the yield of products obtained by the method are high, and the production cost is low. The polymerizable monomer provided by the invention is enabled to be co-polymerized to other monomers, so that an oil-driving polymer with high molecular, high apparent viscosity, excellent heat resistance and excellent salt resistance can be obtained. An oil displacement agent compounded by the polymer and a surfactant has higher stickiness, excellent heat resistance and excellent salt resistance.
Synthesis of thermo- and photo-responsive polysiloxanes with tunable phase separation: Via aza-Michael addition
Feng, Kai,Li, Shusheng,Feng, Linglong,Feng, Shengyu
, p. 14498 - 14504 (2017/11/28)
Two kinds of thermo- and photo-dual-responsive polysiloxanes (DRPSs) with functional pendent groups, N-isopropyl amides and azobenzene (Azo) or salicylideneaniline (SA), were synthesized through a facile, effective, and catalyst-free aza-Michael addition of poly(aminopropylmethyl-siloxane) with N-isopropyl acrylamide and N-azobenzene acrylamide or N-salicylaldehyde acrylamide. The chemical structrures of DRPSs were systematically characterized using FT-IR, H NMR and UV-Vis spectroscopy. The as-prepared DRPSs with lower Azo or SA contents exhibited lower critical solution temperature (LCST)-type phase transition in water, which is reversible and can be controlled by temperature and UV light. The effects of Azo and SA contents on the responsive properties of DRPSs are examined in detail. The LCST decreased with the increasing Azo or SA content. Once the content of Azo or SA reached up to 5.7% or 8.2%, respectively, DRPSs could not be dissolved in water even in an ice bath. Higher values of the LCST were measured after irradiation of the polymer solutions due to the higher polarity of cis-Azo and keto-SA conformation, induced by irradiation. The differences in cloud points between the irradiated and the non-irradiated DRPS aqueous solutions increased up to 3.4 °C and 9.8 °C when combined with 3.8% Azo and 5.8% SA units, respectively.
TANK-BINDING KINASE INHIBITOR COMPOUNDS
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Paragraph 0335; 0336, (2016/05/02)
Compounds having the following formula (I) and methods of their use and preparation are disclosed:
PYRIMIDINE DERIVATIVES AS KINASE INHIBITORS AND THEIR THERAPEUTICAL APPLICATIONS
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, (2016/09/22)
The present invention provides kinase inhibitors with anti-proliferative activity comprising substituted pyrimidine derivatives and pharmaceutically-acceptable formulations thereof. In addition, the invention provides methods for making novel compounds and methods for using the compounds.
INHIBITORS OF CYCLIN-DEPENDENT KINASE 7 (CDK7)
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Paragraph 389, (2015/05/05)
The present invention provides novel compounds of Formula (I) and Formula (II), and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g.,leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g., cyclin-dependent kinase 7 (CDK7)), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject. (I)
Discovery and structure-activity relationship of potent and selective covalent inhibitors of transglutaminase 2 for Huntington's disease
Prime, Michael E.,Andersen, Ole A.,Barker, John J.,Brooks, Mark A.,Cheng, Robert K. Y.,Toogood-Johnson, Ian,Courtney, Stephen M.,Brookfield, Frederick A.,Yarnold, Christopher J.,Marston, Richard W.,Johnson, Peter D.,Johnsen, Siw F.,Palfrey, Jordan J.,Vaidya, Darshan,Erfan, Sayeh,Ichihara, Osamu,Felicetti, Brunella,Palan, Shilpa,Pedret-Dunn, Anna,Schaertl, Sabine,Sternberger, Ina,Ebneth, Andreas,Scheel, Andreas,Winkler, Dirk,Toledo-Sherman, Leticia,Beconi, Maria,MacDonald, Douglas,Mu?oz-Sanjuan, Ignacio,Dominguez, Celia,Wityak, John
, p. 1021 - 1046 (2012/04/10)
Tissue transglutaminase 2 (TG2) is a multifunctional protein primarily known for its calcium-dependent enzymatic protein cross-linking activity via isopeptide bond formation between glutamine and lysine residues. TG2 overexpression and activity have been found to be associated with Huntington's disease (HD); specifically, TG2 is up-regulated in the brains of HD patients and in animal models of the disease. Interestingly, genetic deletion of TG2 in two different HD mouse models, R6/1 and R6/2, results in improved phenotypes including a reduction in neuronal death and prolonged survival. Starting with phenylacrylamide screening hit 7d, we describe the SAR of this series leading to potent and selective TG2 inhibitors. The suitability of the compounds as in vitro tools to elucidate the biology of TG2 was demonstrated through mode of inhibition studies, characterization of druglike properties, and inhibition profiles in a cell lysate assay.