- Conjugated polymers based on 1,8-naphthalene monoimide with high electron mobility
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1,4,8,9-Naphthalene diimides (NDIs) with strong electron accepting ability and high stability are excellent building blocks for semiconductor polymers. However, 1,8-naphthalene monoimide (NMI) with similar structure and energy levels as that of NDI has never been used to construct conjugated polymers because of synthetic difficulty. Herein, 3,6-dibromo-NMI (DBNMI) with bulky alkyl groups was obtained effectively in a four-step synthesis, and three donor-acceptor (D-A) type conjugated polymers based on NMI were firstly prepared. These polymers have strong absorption in the range of 300–600 nm, low LUMO level of 3.68 eV, and moderate bandgaps of 2.18 eV. Space charge limiting current measurements indicate these polymers are typical electron transporting materials, and the highest electron mobility is up to 5.8 × 10?3 cm2?V?1?s?1, which is close to the star acceptor based on NDI (N2200, 5.0 × 10?3 cm2?V?1?s?1).
- Zhu, Guomin,Zhang, Youdi,Hu, Yu,Zhao, Xiaohong,Yuan, Zhongyi,Chen, Yiwang
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- Design, synthesis, biophysical and biological studies of trisubstituted naphthalimides as G-quadruplex ligands
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A series of trisubstituted naphthalimides have been synthesized and evaluated as telomeric G-quadruplex ligands by biophysical methods. Affinity for telomeric G-quadruplex AGGG(TTAGGG)3 binding was first screened by fluorescence titrations. Subsequently, the interaction of the telomeric G-quadruplex with compounds showing the best affinity has been studied by isothermal titration calorimetry and UVmelting experiments. The two best compounds of the series tightly bind the telomeric quadruplex with a 2:1 drug/DNA stoichiometry. These derivatives have been further evaluated for their ability to inhibit telomerase by a TRAP assay and their pharmacological properties by treating melanoma (M14) and human lung cancer (A549) cell lines with increasing drug concentrations. A dose-dependent inhibition of cell proliferation was observed for all cellular lines during short-term treatment.
- Peduto, Antonella,Pagano, Bruno,Petronzi, Carmen,Massa, Antonio,Esposito, Veronica,Virgilio, Antonella,Paduano, Francesco,Trapasso, Francesco,Fiorito, Filomena,Florio, Salvatore,Giancola, Concetta,Galeone, Aldo,Filosa, Rosanna
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Read Online
- Identification of benzo[cd]indol-2(1H)-ones as novel Atg4B inhibitors via a structure-based virtual screening and a novel AlphaScreen assay
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Targeting autophagy is a promising therapeutic strategy for cancer treatment. As a result, the identification of novel autophagy inhibitors is an emerging field of research. Herein, we report the development of a novel AlphaScreen HTS assay that combined
- Quintana, Mireia,Bilbao, Ana,Comas-Barceló, Júlia,Bujons, Jordi,Triola, Gemma
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p. 648 - 666
(2019/06/21)
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- SMALL MOLECULE MODIFIERS OF MICRORNA MIR-122
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MicroRNAs are a class of endogenous regulators of gene function. Aberrant regulation of microRNAs has been linked to various human diseases, most importantly cancer. Small molecule intervention of microRNA misregulation has the potential to provide new th
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Page/Page column 38; 49-50
(2011/08/08)
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- Fluorescent labeling of specific protein targets in vitro and in vivo
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New methods are provided for the post-genomic era that will permit the analysis of the dynamic expression and localization of gene products in living cells. Herein we propose the development of such a method from a bioorganic approach involving organic sy
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- Synthesis and characterization of dimaleimide fluorogens designed for specific labeling of proteins
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A series of aromatic compounds were prepared bearing two maleimide groups attached directly to the fluorescent cores. The resulting derivatives do not fluoresce until the maleimide groups undergo their typical thiol addition reaction, thus removing their
- Girouard, Stephane,Houle, Marie-Helene,Grandbois, Alain,Keillor, Jeffrey W.,Michnick, Stephen W.
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p. 559 - 566
(2007/10/03)
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- Reactions of isomeric dinitronaphthalic-1,8-anhydrides with alkylamines
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In the reaction products of 4,5-dinitronaphthalic-1,8-anhydride and of the 3,6-dinitro analogue with 1-butylamine only nitro groups in the former compound undergo reaction. 2,5-Dinitronaphthalic anhydride reacted partially. 4,5-Dibutylaminonaphthalic-N-butyl-1,8-imide was moderately fluorescent by comparison with 4-butylamino-N-butyl-1,8-imide, (FBYR). The ease of nucleophilic replacement of the nitro group in mononitro substituted rings increases with ring size and appears to be related to the stability of a Meisenheimer intermediate.
- Alexiou,Tyman
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- Isoquinolones
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Benzo[de]isoquinoline-1,3-dione of Formula or a pharmaceutically acceptable salt thereof wherein R is hydrogen or a protecting group typically used in the art for protecting alcohols and R1-R5are each independently chosen from H, Cl, Br, F, straight or branched alkyl C1-C8alkyl, C3-C8cycloalkyl, heterocycle or bridged heterocycle of 4-9 atoms containing 1-3 heteroatoms, —(CR′2)nOR6, —(CR′2)nN(R6)2, —(CR′2)nNR6COR7, —(CR′2)nNR6SO2OR7, —(CR′2)nNR6SO2N(R6)2, —(CR′2)nOSO2N(R6)2, —(CR′2)nCN, —(CR′2)n(NOR6)R7, NO2, CF3, —(CR′2)nSOmR7, —(CR′2)nSOmR7, —(CR′2)nCO2R6, —(CR′2)nCON(R6)2, Ph, and any two of R1-R5may form a substituted or unsubstituted ring of 5-7 total atoms having 0-2 heteroatoms are claimed which are selective inhibitors of bacterial DNA gyrase and DNA topoisomerase useful in antibacterial agents. Methods for their preparation and formulation as well as novel intermediates useful in the preparation of the final products are also claimed.
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- Synthesis, structure and antitumor activity of new benz[d,e]isoquinoline-1,3-diones
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New benz[d,e]isoquinoline-1,3-diones related to mitonafide (CAS 54824-17-8) and amonafide (CAS 69408-81-7) with double substitution on the chromophore and branched side chains have been synthesized and their biological activity determined. Molecular modeling studies of 3a based on X-ray crystallographic data of mitonafide have shown that the aromatic system intercalates between GC steps of DNA. The in vitro cytotoxic test data using CX-1 and LX-1 cells showed higher cytotoxic activities in disubstituted derivatives compared to both lead compounds. Some of the compounds have been selected for in vivo test using L1210 tumor cells and CX-1 cells. Two of them (3b and 3j) have shown promising activity as good candidates for clinical development.
- Brana,Castellano,Moran,Emling,Kluge,Schlick,Klebe,Walker
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p. 1311 - 1318
(2007/10/02)
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