- Organic Nanotube with Subnanometer, pH-Responsive Lumen
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While many synthetic nanotubes with a hydrophobic lumen and fast molecular transport have been developed, decorating the interior of these channels with polar and/or responsive functional groups remains challenging. In transmembrane proteins like the aqua
- Darnall, Shawn M.,Li, Changyi,Dunbar, Martha,Alsina, Marco,Keten, Sinan,Helms, Brett A.,Xu, Ting
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supporting information
p. 10953 - 10957
(2019/08/07)
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- Synthesis, characterization of benzimidazole carboxamide derivatives as potent anaplastic lymphoma kinase inhibitor and antioxidant activity
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Novel benzimidazole carboxamide derivatives have been synthesized and characterized by FTIR, NMR, and mass spectral analysis. The synthesized compounds 7a, 7d, and 7f showed excellent scavenging capacity against DPPH radical and the results are comparable with ascorbic acid. In-silico molecular docking studies exhibited compounds 7a, 7d, and 7f had a good affinity towards the active pocket and the results indicated the ability of potent and selective inhibition of anaplastic lymphoma kinase (ALK) receptor. The theoretical investigation of MEPs, HOMO, LUMO, and the energy gap of HOMO-LUMO were calculated by B3LYP/6-31G method and reactivity descriptors were also computed.
- Sam Daniel Prabu,Lakshmanan, Sivalingam,Ramalakshmi,Thirumurugan,Govindaraj, Dharman,Antony, S. Arul
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p. 266 - 278
(2019/01/19)
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- Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a] quinoxaline derivatives as inhibitors of the human protein kinase CK2
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Herein we describe the synthesis and properties of substituted phenylaminopyrrolo[1,2-a]quinoxaline-carboxylic acid derivatives as a novel class of potent inhibitors of the human protein kinase CK2. A set of 15 compounds was designed and synthesized using
- Guillon, Jean,Le Borgne, Marc,Rimbault, Charlotte,Moreau, Stéphane,Savrimoutou, Solène,Pinaud, No?l,Baratin, Sophie,Marchivie, Mathieu,Roche, Séverine,Bollacke, Andre,Pecci, Adali,Alvarez, Lautaro,Desplat, Vanessa,Jose, Joachim
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p. 205 - 222
(2013/10/01)
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- INTERMEDIATE COMPOUNDS FOR THE PREPARATION OF ANGIOTENSIN II ANTAGONISTS
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The present invention relates to novel substituted biphenyltetrazole compounds useful as intermediates in the preparation of angiotensin II antagonists, to a process for the synthesis of them and to a process for the conversion thereof to said molecules.
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Page/Page column 25; 38
(2010/11/30)
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- IMIDAZO(1,2-a)PYRIDINE DERIVATIVE
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A compound reprsented by the following formula (I), its salts or nsolvates thereof capable of specifically or selectively expressig an antifungal activity in a broad spectrum based on the novel mechanism thereof of 1,6-β-glucan synthesis inhibition, and an antifungal agent containing any of them.
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Page 106; 107
(2010/02/09)
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- Cyclo-alkyl substituted benzimidazoles and their use as PARP inhibitors
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Compounds of the formula I or II and their tautomeric forms, possible enantiomeric and diastereomeric forms, possible cistrans isomers on the rings in A and prodrugs thereof, pharmaceutical compositions containing these compounds and methods of treating neurodegenerative diseases or neuronal damage with these compounds.
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Page column 10
(2008/06/13)
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- Quinoxaline biphenyl angiotensin II inhibitors
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Angiotensin II inhibition is exhibited by STR1 wherein: X is --CH2 -- or O; R is hydrogen, alkyl, aryl, cycloalkyl, aralkyl, or cycloalkylalkyl; R1 and R2 are each independently O or absent; R3 is hydrogen, alkyl, alkenyl, alkoxy, cycloalkyl, aryl, aralkyl, cycloalkylalkyl, halo, haloalkyl, or haloalkoxy; R4 is hydrogen, alkyl, alkenyl, alkoxy, aryl, cycloalkyl, aralkyl, cycloalkylalkyl, --R8 --OH, or --R8 CO2 R9 ; and the remaining symbols are as defined in the specification.
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- Potential Antitumor Agents. 59. Structure-Activity Relationships for 2-Phenylbenzimidazole-4-carboxamides, a New Class of "Minimal" DNA-Intercalating Agents Which May Not Act via Topoisomerase II
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A series of substituted 2-phenylbenzimidazole-4-carboxamides has been synthesized and evaluated for in vitro and in vivo antitumor activity.These compounds represent the logical conclusion to our search for "minimal" DNA-intercalating agents with the lowest possible DNA-binding constants.Such "2-1" tricyclic chromophores, of lower aromaticity than the structurally similar 2-phenylquinolines, have the lowest DNA binding affinity yet seen in the broad series of tricyclic carboxamide intercalating agents.Despite very low in vitro cytotoxicities, several of the compoundshad moderate levels of in vivo antileukemic effects.However, the most interesting aspect of their biological activity was the lack of cross-resistance shown to an amsacrine-resistant P388 cell line, suggesting that these compounds may not express their cytotoxicity via interaction with topoisomerase II.
- Denny, William A.,Rewcastle, Gordon W.,Baguley, Bruce C.
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p. 814 - 819
(2007/10/02)
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