1428673-20-4Relevant articles and documents
Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX
Dudutiene, Virginija,Matuliene, Jurgita,Smirnov, Alexey,Timm, David D.,Zubriene, Asta,Baranauskiene, Lina,Morkunaite, Vaida,Smirnoviene, Joana,Michailoviene, Vilma,Juozapaitiene, Vaida,Mickevi?iute, Aurelija,Kazokaite, Justina,Bak?yte, Sandra,Kasiliauskaite, Aiste,Jachno, Jelena,Revuckiene, Jurgita,Ki?onaite, Migle,Pilipuityte, Vilma,Ivanauskaite, Egle,Milinavi?iute, Goda,Smirnovas, Vytautas,Petrikaite, Vilma,Kairys, Visvaldas,Petrauskas, Vytautas,Norvai?as, Povilas,Linge, Darius,Gibie?a, Paulius,?apkauskaite, Edita,Zak?auskas, Audrius,Kazlauskas, Egidijus,Manakova, Elena,Gra?ulis, Saulius,Ladbury, John E.,Matulis, Daumantas
, p. 9435 - 9446 (2014)
Human carbonic anhydrase IX (CA IX) is highly expressed in tumor tissues, and its selective inhibition provides a potential target for the treatment of numerous cancers. Development of potent, highly selective inhibitors against this target remains an unmet need in anticancer therapeutics. A series of fluorinated benzenesulfonamides with substituents on the benzene ring was designed and synthesized. Several of these exhibited a highly potent and selective inhibition profile against CA IX. Three fluorine atoms significantly increased the affinity by withdrawing electrons and lowering the pKa of the benzenesulfonamide group. The bulky ortho substituents, such as cyclooctyl or even cyclododecyl groups, fit into the hydrophobic pocket in the active site of CA IX but not CA II, as shown by the compound's co-crystal structure with chimeric CA IX. The strongest inhibitor of recombinant human CA IX's catalytic domain in human cells achieved an affinity of 50 pM. However, the high affinity diminished the selectivity. The most selective compound for CA IX exhibited 10 nM affinity. The compound that showed the best balance between affinity and selectivity bound with 1 nM affinity. The inhibitors described in this work provide the basis for novel anticancer therapeutics targeting CA IX.
COLORING COMPOSITION, CURED FILM, COLOR FILTER, METHOD FOR PRODUCING COLOR FILTER, SOLID-STATE IMAGING ELEMENT, AND IMAGE DISPLAY DEVICE
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, (2017/09/19)
Provided are a coloring composition having improved heat resistance; and a cured film, a color filter, a method for producing a color filter, and a solid-state imaging element and an image display device, each of which uses the coloring composition. The coloring composition includes a dye (A) represented by the following General Formula (I) and a polymerizable compound (B). In General Formula (I), Q represents an (m+n)-valent linking group, R represents a substituent, represents a dye residue, m represents an integer of 0 to 6, n represents an integer of 2 to 8, and (m+n) represents an integer of 2 to 8. In the case where m is 2 or more, a plurality of R's may be different from each other, and in the case where n is 2 or more, a plurality of D's may be different from each other. (R)m-Q-(D)n??General Formula(I)
Colored composition, cured film, color filter, color-filter manufacturing method, solid-state imaging element, image display device, polymer, and xanthene dye
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Paragraph 0837, (2016/10/09)
This colored composition contains a curable compound, a solvent, and a dye compound that has a dye structure having a cationic portion and an anionic portion that contains at least one of the following: a structure that can be represented by general formula (A1); a structure that can be represented by general formula (A2); and a structure that contains a boron atom. The aforementioned cationic and anionic portions of the dye structure of the dye compound are covalently bound together in the same molecule. General formula (A1) In general formula (A1), R1 and R2 each independently represent either -SO2- or -CO-. General formula (A2) In general formula (A2), R3 represents either -SO2- or -CO- and R4 and R5 each independently represent -SO2-, -CO-, or -CN.
COLORING COMPOSITION, CURED FILM, COLOR FILTER, MANUFACTURING METHOD FOR COLOR FILTER, SOLID STATE IMAGING ELEMENT, AND IMAGE DISPLAY DEVICE
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, (2016/10/10)
PROBLEM TO BE SOLVED: To provide a coloring composition with which it is possible to solve planar irregularities, and a cured film, a color filter, a method for producing a color filter, a solid state imaging element, and an image display device using the coloring composition. SOLUTION: A coloring composition contains a pigment compound represented by the left formula, a curable compound, and a solvent, the pigment compound represented by the left formula having a counter anion inside and/or outside the molecule, wherein one of Ar1 and Ar2 is a group represented by the right formula; the other is a hydrogen atom, a group represented by the right formula, or the like; R5 and R6 independently represent hydrogen atoms or the like; R7 represents a monovalent substituent; R8 represents a halogen atom or the like; p is an integer from 0 to 4; R1 and R2 independently represent alkyl groups having 3 or more carbon atoms or the like; X1 to X3 independently represent hydrogen atoms or the like. COPYRIGHT: (C)2015,JPOandINPIT
4-Substituted-2,3,5,6-tetrafluorobenzenesulfonamides as inhibitors of carbonic anhydrases I, II, VII, XII, and XIII
Dudutiene, Virginija,Zubriene, Asta,Smirnov, Alexey,Gylyte, Joana,Timm, David,Manakova, Elena,Gra?ulis, Saulius,Matulis, Daumantas
, p. 2093 - 2106 (2013/04/24)
A series of 4-substituted-2,3,5,6-tetrafluorobenezenesulfonamides were synthesized and their binding potencies as inhibitors of recombinant human carbonic anhydrase isozymes I, II, VII, XII, and XIII were determined by the thermal shift assay, isothermal
