- Fluorescent-labeled excision type nucleotide, synthetic method and application of fluorescent-labeled excision type nucleotide in DNA sequencing
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The invention relates to a fluorescent-labeled excision type nucleotide. The fluorescent-labeled excision type nucleotide is characterized by comprising a structure as shown in the general formula (I), wherein in the general formula (I), Fluorescent repre
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Paragraph 0088; 0090-0094
(2018/11/27)
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- Indazole-oxadiazole derivative, medicinal composition containing derivative, and application of derivative in tumor prevention
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The invention discloses an indazole-oxadiazole derivative with the structure represented by general formula a shown in the description, or a pharmaceutically acceptable salt or solvate thereof. In the formula, X is O or N, Y is N, Z is N or O, and all groups are as defined in the description. The invention also discloses a medicinal composition adopting the derivative as an active component, and a use of the derivative. Compounds synthesized in the invention have an HIF-1 inhibition effect, and most of the compounds have a substantial HIF-1 inhibition effect, have strong in-vivo and in-vitro anti-HIF-1 effect on human colorectal carcinoma cell strains (HCT116) and other tumor cell strains, and can be used for treating tumor diseases.
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Paragraph 0229; 0230; 0231
(2017/07/25)
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- A 4 + 4 strategy for synthesis of zeolitic metal-organic frameworks: An indium-MOF with SOD topology as a light-harvesting antenna
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A zeolitic metal-organic framework with a SOD topology, (Et 2NH2)[In(BCBAIP)]·4DEF·4EtOH (H 4BCBAIP: 5-(bis(4-carboxybenzyl)amino)isophthalic acid) (1), has been constructed by a 4 + 4 synthetic strategy from tetrahedral organic building units and In3+ ions. Compound 1 could adsorb organic dyes and be used as a light-harvesting antenna.
- Sun, Libo,Xing, Hongzhu,Liang, Zhiqiang,Yu, Jihong,Xu, Ruren
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p. 11155 - 11157
(2013/11/19)
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- HISTONE DEACETYLASE INHIBITORS
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The disclosure provides compounds of formula I and methods for preparation thereof. The compounds act as inhibitor of histone deacetylase.
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Page/Page column 22
(2012/05/04)
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- HISTONE DEACETYLASE INHIBITORS
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The disclosure provides compounds of formula I and methods for preparation thereof. The compounds act as inhibitor of histone deacetylase.
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Page/Page column 57; 58
(2011/04/13)
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- Synthesis and evaluation of 5-substituted 9-hydroxypyrrolo[3,4-c]carbazole- 1,3(2H,6H)-diones as check point 1 kinase inhibitors
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The structure-activity relationship (SAR) of 5-substituted pyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione derivatives 5 was investigated for their potential as Chk1 inhibitors for possible chemo- and radio-potentiators in anticancer chemotherapies. In silico vi
- Sako, Yuki,Ichikawa, Satoshi,Osada, Akiko,Matsuda, Akira
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experimental part
p. 7878 - 7889
(2011/02/23)
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- N-benzyl substituted pyridyl porphyrin compounds and methods of use thereof
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The present invention relates to N-Benzyl-Substituted Pyridyl Porphyrin Compounds, compositions comprising an effective amount of an N-Benzyl-Substituted Pyridyl Porphyrin Compound and methods for treating or preventing injury due to exposure to a reactiv
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Page/Page column 32-33
(2010/11/26)
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- Extended peptoids: a new class of oligomers based on aromatic building blocks
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Peptoids (N-substituted polyglycines) represent a class of bioinspired oligomers that have unique physical and structural properties. Here, we report the construction of 'extended peptoids' based on aromatic building blocks, in which the N-alkylaminoacetyl group of the peptoid backbone has been replaced by an N-alkylaminomethylbenzoyl spacer. Both meta- and para-bromomethylbenzoic acids were synthesized, providing access to a new class of peptoids. Further, inclusion of hydrophilic side chains confers water solubility to these compounds, showing that, like simple peptoids, extended peptoids add an extra dimension to synthetic poly-amide oligomers with potential application in a variety of biological contexts.
- Combs, David J.,Lokey, R. Scott
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p. 2679 - 2682
(2008/02/03)
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- PYRIDYL-SUBSTITUTED PORPHYRIN COMPOUNDS AND METHODS OF USE THEREOF
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The present invention relates to Pyridyl-Substituted Porphyrin Compounds, compositions comprising an effective amount of a Pyridyl-Substituted Porphyrin Compound and methods for treating or preventing injury due to exposure to a reactive species, erectile dysfunction due to surgery, lung disease, hyperoxia, neurodegenerative disease, liver disease, myocardial damage during cardioplegia, an inflammatory condition, a reperfusion injury, an ischemic condition, a cardiovascular disease, diabetes, a diabetic complication, cancer, a side effect of cancer chemotherapy, or a radiation-induced injury, or to prolong the half-life of an oxidation-prone compound, comprising administering to a subject in need thereof an effective amount of a Pyridyl-Substituted Porphyrin Compound.
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Page/Page column 79-80
(2008/06/13)
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- Reparametrization and/or determination of hammett, inductive, mesomeric and aise substituent constants for five substituents: N+(CH 3)3, CH2N+(CH3) 3, CH2Py+, CH2SO2CH 3 and PO(OCH3)2
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Ten meta- and para-substituted benzoic acids with substituants N +(CH3)3, CH2N+(CH 3)3, CH2Py+, CH2SO 2CH3 and PO(OCH3)2 were synthesized. Dissociation constants of these acids were determined in five solvents (water, ethanol, methanol, N,N-dimethylformamide, dimethyl sulfoxide) at 25°C. Dissociation constants of benzoic acid derivatives with other substituents H, CH3, NHCOCH3, OCH3, F, Cl, Br, I, COCH 3, CN, NO2, SO2CH3 were taken from the literature (calibration set). Substituent constants σm, σp, σI, σR, and σi for substituents N+(CH3)3, CH2N+(CH3)3, CH2Py +, CH2SO2CH3, and PO(OCH 3)2 were calculated by non-linear and PLS (partial least-square method with latent variables) calibration in three correlation models using the calibration set. Nonlinear regression appears more suitable and more universal than PLS calibration. The advantage of nonlinear regression is its independence on possibly missing data in the given solvent, evaluation of precision (standard deviation), the accessibility of necessary software, and easy calculation. However, in contrast to PLS calibration, this procedure fails in calculation of substituent constants with description of properties of substituents (substituent constants σI, σR). The obtained values of substituent constants are in good agreement with those published in the literature.
- Picha, Jan,Cibulka, Radek,Liska, Frantisek,Parik, Patrik,Pytela, Oldrich
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p. 2239 - 2252
(2007/10/03)
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- Nucleophilic de-coordination and electrophilic regeneration of "hemilabile" pincer-type complexes: Formation of anionic dialkyl, diaryl, and dihydride PtII complexes bearing no stabilizing π-acceptors
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Novel anionic dialkyl, diaryl, and dihydride platinum(II) complexes based on the new πlong-armπ hemilabile PCN-type ligand C6H 4[CH2P(tBu)2](CH2) 2N(CH3)2 with the general formula Li + [Pt(PCN)(R)2]- (R = Me (4), Ph (6) and H (9)) were prepared by reaction of [Pt(PCN)(R)] complexes (obtained from the corresponding chlorides) with an equivalent of RLi, as a result of the opening of the chelate ring. Alkylating agents based on other metals produce less stable products. These anionic d8 complexes are thermally stable although they bear no stabilizing π acceptors. They were characterized by 1H, 31P{1H}, 13C, and 7Li NMR spectroscopy; complex 9 was also characterized by single crystal X-ray crystallography, showing that the Li + ion is coordinated to the nitrogen atom of the open amine arm and to the hydride ligand (trans to the P atom) of a neighboring molecule (H-Li = 2.15 A), resulting in a dimeric structure. Complexes 4 and 9 exhibit high nucleophilic reactivity, upon which the pincer complex is regenerated. Reaction of 4 with water, methyl iodide, and iodobenzene resulted in the neutral complex [Pt(PCN)(CH3)] (3) and methane, ethane, or toluene, respectively. Labeling studies indicate that the reaction proceeds by direct electrophilic attack on the metal center, rather than attack on the alkyl ligand. The anionic dihydride complex 9 reacted with water and methyl iodide to yield [Pt(PCN)(H)] (8) and H2 or methane, respectively.
- Poverenov, Elena,Gandelman, Mark,Shimon, Linda J. W.,Rozenberg, Haim,Ben-David, Yehoshoa,Milstein, David
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p. 4673 - 4684
(2007/10/03)
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- Parallel synthesis of glycomimetic libraries: targeting a C-type lectin.
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We have developed methods for the parallel synthesis of two libraries of non-carbohydrate-based analogues of mannose on a solid support. The natural product shikimic acid was used as a key building block. The ability of the compounds to block the binding of the C-type lectin MBP-A to a mannosylated surface was assessed in a high-throughput assay. Ten library members with inhibitory activities equivalent to that of alpha-methyl mannopyranoside were identified. [reaction: see text]
- Schuster, Michael C,Mann, David A,Buchholz, Tonia J,Johnson, Kathryn M,Thomas, William D,Kiessling, Laura L
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p. 1407 - 1410
(2007/10/03)
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- Protease inhibitors
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The present invention provides compounds of formula (I) which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia or malignancy; and metabolic bone disease therewith.
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- Syntheses of Reactive Fluorescent Stains Derived from 5(2)-Aryl-2(5)-(4-pyridyl)oxazoles and Bifunctionally Reactive Linkers
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Several bifunctionally reactive linkers containing halide or sulfonate ester groups were prepared.The linkers were used to quaternize 5-(4-methoxyphenyl)-2-(4-pyridyl)oxazole and 2-(6-chromanyl)-5-(4-pyridyl)oxazole to produce fluorescent stains that contained a reactive group such as an isothiocyanate, an N-hydroxysuccinimidyl ester, a maleimide, or an oxirane.The stains were derivatized with either 1-propyl-amine, 1-propanethiol, or piperidine, as appropriate, to help in characteriazation.The stains may serve as more photostable alternatives to fluoresceins or coumarins.
- Litak, Peter T.,Kauffman, Joel M.
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p. 457 - 480
(2007/10/02)
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- Synthesis and Characterization of Blocked and Ligand-Appended Hemes Derived from Atropisomeric meso-Diphenylporphyrins
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The synthesis of a series of sterically blocked and imidazole-appended meso-diphenyletioporphyrins is described.These hybrid porphyrins have good solubility and spectroscopic properties of β-substituted porphyrins as well as the orientation specificity of ortho-position-derivatized tetraphenylporphyrins.The effectiveness of the blocking groups is demonstrated by ferric hemin hydroxide formation in the doubly protected trans-5,15-bis-2,8,12,18-tetraethyl-3,7,13,17-tetramethylporphine, characterized by UV-visible, 1H NMR, and IR spectra and cyclic voltammetry.The advantage of the m-benzyl linkage in enforcing imidazole coordination to ferric hemes is demonstrated by 1H NMR studies on various type of imidazole-appended heme complexes.Several potential binucleating systems have also been prepared by incorporating nonheme chelating ligands to the hybrid porphyrins.
- Young, Richard,Chang, C. K.
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p. 898 - 909
(2007/10/02)
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