- MATTER OF COMPOSITION, SYNTHESIS, FORMULATION AND APPLICATION OF FL118 PLATFORM POSITIONS 7 AND 9-DERIVED ANALOGUES FOR TREATMENT OF HUMAN DISEASE
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Described herein, are the chemical synthesis, matter of compositions, formulation, function, methods and uses of the FL118 platform Positions 7 and/or 9-derived analogues for treating cancer or other human diseases. Compounds derived from chemical modifications of the FL118 platform are employed alone or in combination with other anti-cancer agents to preclude, eliminate or reverse cancer phenotypes. This invention intends to realize unique personalized cancer treatment (personalized precision medicine) through application of a series of structural relevant individual FL118 platform-derived analogues, which target multiple cellular human disease-relevant proteins and their signaling pathways.
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Paragraph 000118; 000119
(2020/04/25)
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- A Photoactivatable Formaldehyde Donor with Fluorescence Monitoring Reveals Threshold to Arrest Cell Migration
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Controlled light-mediated delivery of biological analytes can enable the investigation of highly reactivity molecules within living systems. As many biological effects are concentration dependent, it is critical to determine the location, time, and quantity of analyte donation. In this work, we have developed the first photoactivatable donor for formaldehyde (FA). Our optimized photoactivatable donor, photoFAD-3, is equipped with a fluorescence readout that enables monitoring of FA release with a concomitant 139-fold fluorescence enhancement. Tuning of photostability and cellular retention enabled quantification of intracellular FA release through cell lysate calibration. Application of photoFAD-3 uncovered the concentration range necessary for arresting wound healing in live cells. This marks the first report where a photoactivatable donor for any analyte has been used to quantify intracellular release.
- Chan, Jefferson,Ibarra, Gabriela E.,Krishnamurthy, Vishnu,Pino, Nicholas W.,Smaga, Lukas P.
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supporting information
(2020/01/31)
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- METHODS AND COMPOSITIONS
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The invention relates to genetic incorporation of 2,3-diamino propionic acid (DAP) into polypeptides, to unnatural amino acids comprising DAP, to a tRNA synthetase for charging tRNA with unnatural amino acids comprising DAP, and to methods of using the resulting polypeptides, for example in capturing substrates and/or intermediates in enzymatic reactions. The invention also relates to compounds of formula (I) or (II): or salts, solvates, tautomers, isomers or mixtures thereof.
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Page/Page column 66; 69; 70
(2020/05/29)
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- Camptothecin derivative and preparation method and application thereof
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The invention relates to a compound with a structure shown in a formula (I), a stereoisomer of the compound and a pharmaceutically acceptable salt form of the compound, and further relates to a preparation method of the compound, a pharmaceutical composition containing therapeutically effective dose of the compound, and application of the pharmaceutical composition in the preparation for the prevention and/or treatment of cancer. The compound is a camptothecin derivative with a novel structure with 10 site and 11 site of a stem nucleus introduced with methylene dioxy groups and 7-site introduced with different substituted groups. The raw materials of the preparation method can be obtained easily, a synthetic method is simple, a purification method is simple and fast, the compound has excellent cytotoxic activity in vitro and excellent antitumor effect in vivo, and the compound has broad medicinal prospects.(Please see the specification for the formula).
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Paragraph 0073-0076
(2020/01/03)
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- COMPOUND, SUBSTRATE FOR PATTERN FORMATION, PHOTODEGRADABLE COUPLING AGENT, PATTERN FORMATION METHOD, AND TRANSISTOR PRODUCTION METHOD
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Provided is a compound represented by Formula (1).
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Paragraph 0177-0180
(2019/12/02)
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- Photogenerated reagents
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This invention describes reagent precursors and methods for chemical and biochemical reactions. These reagent precursors that can be activated in solution upon irradiation to generate reagents required for the subsequent chemical reactions. Specifically, photogenerated reagents (PGR) are useful for controlling parallel combinatorial synthesis and various chemical and biochemical reactions.
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Page/Page column 24
(2008/06/13)
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- Protection and labelling of thymidine by a fluorescent photolabile group
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A fluorescent photolabile group including coumarin and MeNPOC moieties was synthesized to protect 5′-OH terminal function of thymidine (T). Its photochemical and photophysical properties were studied, in particular the photocleavage (photodeprotection under a 365-nm irradiation) is only lowered by a factor of two by addition of the fluorophore. Fluorescence properties of the coumarin probe are not changed upon irradiation, which is satisfactory for the application required, i.e., in situ synthesis of DNA microarrays.
- Muller, Caroline,Even, Pascale,Viriot, Marie-Laure,Carre, Marie-Christiane
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p. 3735 - 3741
(2007/10/03)
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- Camptothecin compounds with combined topoisomerase I inhibition and DNA alkylation properties
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Camptothecin compounds having a --CH2 --L group are effective anti-tumor compounds. These compounds inhibit the enzyme topoisomerase I and DNA of associated topoisomerase I-DNA complexes.
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- Pentadienylnitrobenzyl and Pentadienylnitropiperonyl Photochemically Removable Protecting Groups
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New photochemically removable protecting groups have been developed based on classical nitrobenzyl compounds modified by the inclusion of a pentadienyl group. It serves to trap through an internal Diels-Alder reaction the nitroso group produced as part of the photochemical deprotection process, preventing its further photochemistry or chemical reactions with nucleophiles.
- Pirrung, Michael C.,Lee, Yong Rok,Park, Kaapjoo,Springer, James B.
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p. 5042 - 5047
(2007/10/03)
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- The efficiency of light-directed synthesis of DNA arrays on glass substrates
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New methods based on photolithography and surface fluorescence were used to determine photodeprotection rates and stepwise yields for light-directed oligonucleotide synthesis using photolabile 5'-(((α-methyl-2- nitropiperonyl)-oxy)carbonyl)(MeNPOC)-2'-deoxynucleoside phosphoramidites on planar glass substrates. Under near-UV illumination (primarily 365 nm) from a mercury light source, the rate of photoremoval of the MeNPOC protecting group was found to be independent of both the nucleotide and length of the growing oligomer (t( 1/4 ) = 12 s at 27.5 mW/cm2). A moderate dependence on solvent polarity was observed, with photolysis proceeding most rapidly in the presence of nonpolar solvents or in the absence of solvent (e.g., t( 1/4 ) = 10 - 13 s at 27.5 mW/cm2). In solution, the photolysis rate was linearly dependent on light intensity over the range 5-50 mW/cm2. Average stepwise yields for the synthesis of dodecamer oligonucleotides were in the range of 92-94%, using monomers based on N6-(phenoxyacetyl)-2'-deoxyadenosine, N2- isobutyryl-2'-deoxyguanosine, N4-isobutyryl-2'-deoxycytidine, and thymidine. By comparison, an efficiency of 98%/step was obtained using a conventional 5'-dimethoxytrityl monomer with acid deprotection on the same support. The lower yields associated with the photochemical process appears to be due to incomplete recovery of free 5'-hydroxyl groups after photolysis on the support, although high yields of 5'-OH nucleosides (≤96%) are consistently observed when 5'-MeNPOC monomers are photolyzed in solution.
- McGall, Glenn H.,Barone, Anthony D.,Diggelmann, Martin,Fodor, Stephen P. A.,Gentalen, Erik,Ngo, Nam
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p. 5081 - 5090
(2007/10/03)
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- Facile synthesis of a o-nitrobenzyl photolabile linker for combinatorial chemistry
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Two facile syntheses are described of the o-nitrobenzyl alcohol photolabile linker (5). This compound is a valuable intermediate in the preparation of combinatorial libraries, where it allows release from the solid support to give libraries of acids.
- Teague, Simon J.
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p. 5751 - 5754
(2007/10/03)
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