- Functionalized defects through solvent-assisted linker exchange: Synthesis, characterization, and partial postsynthesis elaboration of a metal-organic framework containing free carboxylic acid moieties
-
Intentional incorporation of defect sites functionalized with free carboxylic acid groups was achieved in a paddlewheel-based metal-organic framework (MOF) of rht topology, NU-125. Solvent-assisted linker exchange (SALE) performed on a mixed-linker deriva
- Karagiaridi, Olga,Vermeulen, Nicolaas A.,Klet, Rachel C.,Wang, Timothy C.,Moghadam, Peyman Z.,Al-Juaid, Salih S.,Stoddart, J. Fraser.,Hupp, Joseph T.,Farha, Omar K.
-
-
Read Online
- Benzene tricarboxamide derivatives with lipid and ethylene glycol chains self-assemble into distinct nanostructures driven by molecular packing
-
The self-assembly in aqueous solution of benzene-1,3,5-tricarboxamide (BTA) bearing one alkyl chain and two PEG (polyethylene glycol) chains or two alkyl chains and one PEG chain yields completely distinct nanostructures. Two series of derivatives were sy
- Aljuaid, Nada,Hamley, Ian W.,Ruokolainen, Janne,Seitsonen, Jani,Tully, Mark
-
supporting information
p. 8360 - 8363
(2021/08/25)
-
- Silica-Mediated Monohydrolysis of Dicarboxylic Esters
-
A new method for the monohydrolysis of dicarboxylic esters is presented, involving as key step a silanolysis at elevated temperatures at the silica gel surface. In the second step, the surface bound silyl esters are cleaved off under mild conditions, giving a straightforward and fast access to half esters. Based on recovered starting material generally yields well above 70 % are achieved, both, with stiff aromatic as well as flexible aliphatic substrates, as long as the ester groups involved are remote enough from each other. Otherwise competing reactions are becoming determinative, anhydride formation in the case of phthalates and decarbonylative fragmentation in the case of malonates. The new method was also successfully tested on a multigram scale with a minimalistic apparatus setup.
- Dyker, Gerald
-
supporting information
p. 6773 - 6776
(2021/12/31)
-
- CYTOTOXIC BIS-BENZODIAZEPINE DERIVATIVES AND CONJUGATES THEREOF WITH CELL-BINDING AGENTS FOR INHIBITING ABNORMAL CELL GROWTH OR FOR TREATING PROLIFERATIVE DISEASES
-
The invention relates to benzodiazepine derivatives with antiproliferative activity and more specifically to benzodiazepine compounds of formulae (I), (II), (TI) and (T2). The invention also provides conjugates of the benzodiazepine compounds linked to a
- -
-
Paragraph 00265
(2020/10/20)
-
- AMINOGUANIDINE HYDRAZONES AS RETROMER STABILIZERS USEFUL FOR TREATING NEUROLOGICAL DISEASES
-
The present invention relates to novel aminoguanidine hydrazone-derivatives of Formula (I) which are effective as retromer stabilizers and useful as neuroprotecting drugs. The invention also relates to pharmaceutical compositions comprising the compounds and their use in therapy and diagnostic.
- -
-
Page/Page column 24; 60
(2020/10/20)
-
- Peptidomimetic plasmepsin inhibitors with potent anti-malarial activity and selectivity against cathepsin D
-
Following up the open initiative of anti-malarial drug discovery, a GlaxoSmithKline (GSK) phenotypic screening hit was developed to generate hydroxyethylamine based plasmepsin (Plm) inhibitors exhibiting growth inhibition of the malaria parasite Plasmodium falciparum at nanomolar concentrations. Lead optimization studies were performed with the aim of improving Plm inhibition selectivity versus the related human aspartic protease cathepsin D (Cat D). Optimization studies were performed using Plm IV as a readily accessible model protein, the inhibition of which correlates with anti-malarial activity. Guided by sequence alignment of Plms and Cat D, selectivity-inducing structural motifs were modified in the S3 and S4 sub-pocket occupying substituents of the hydroxyethylamine inhibitors. This resulted in potent anti-malarials with an up to 50-fold Plm IV/Cat D selectivity factor. More detailed investigation of the mechanism of action of the selected compounds revealed that they inhibit maturation of the P. falciparum subtilisin-like protease SUB1, and also inhibit parasite egress from erythrocytes. Our results indicate that the anti-malarial activity of the compounds is linked to inhibition of the SUB1 maturase plasmepsin subtype Plm X.
- Zogota, Rimants,Kinena, Linda,Withers-Martinez, Chrislaine,Blackman, Michael J.,Bobrovs, Raitis,Pantelejevs, Teodors,Kanepe-Lapsa, Iveta,Ozola, Vita,Jaudzems, Kristaps,Suna, Edgars,Jirgensons, Aigars
-
supporting information
p. 344 - 352
(2018/12/11)
-
- COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USE THEREOF AS INHIBITORS OF RAN GTPASE
-
Compounds of general formula IA, IB and IC outlined below, including pharmaceutically acceptable salts, solvates and hydrates thereof. Such compounds and pharmaceutical compositions comprising them may be used in medical conditions involving Ran GTPase.
- -
-
Paragraph 00106
(2019/04/09)
-
- Adsorbed film type imidazoline corrosion inhibitor and preparing method thereof
-
The invention discloses an adsorbed type imidazoline corrosion inhibitor and a preparing method thereof. The structural formula of the imidazoline corrosion inhibitor is shown in the description, wherein R is linear-chain or branched-chain hydrocarbon or
- -
-
Paragraph 0030; 0038; 0046; 0054
(2017/04/29)
-
- CYTOTOXIC BENZODIAZEPINE DERIVATIVES
-
The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VI). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.
- -
-
Paragraph 0519
(2016/04/19)
-
- POTENT AND SELECTIVE INHIBITORS OF NAV1.7
-
Disclosed is a composition of matter comprising an isolated polypeptide, which is a peripherally-restricted NaV1.7 inhibitor. In some disclosed embodiments, the isolated polypeptide is an inhibitor of NaV1.7. Other embodiments are co
- -
-
Paragraph 1043-1044
(2016/02/18)
-
- ANTHRACENYL-TETRALACTAM MACROCYCLES AND THEIR USE IN DETECTING A TARGET SACCHARIDE
-
A water-soluble compound of the formula (I): (Formula (I)) wherein R9 and R10 are suitably hydrophilic substituents, which may be used to selectively bind to a target saccharide such as glucose and which exhibits a detectable spectro
- -
-
Paragraph 0229
(2015/06/03)
-
- ANTHRACENYL - TETRALACTAM MACROCYCLES AND THEIR USE IN DETECTING A TARGET SACCHARIDE
-
A water-soluble compound of the formula (I): (Formula (I)) wherein R9 and R10 are suitably hydrophilic substituents, which may be used to selectively bind to a target saccharide such as glucose and which exhibits a detectable spectroscopic response to such binding, thus enabling its use in the detection and correction of blood glucose concentrations in vivo.
- -
-
Page/Page column 50
(2013/11/18)
-
- Symmetry breaking in the self-assembly of partially fluorinated benzene-1,3,5-tricarboxamides
-
The interplay of two subsequent aggregation processes results in a symmetry-breaking phenomenon in an achiral self-assembling system. Partially fluorinated benzene-1,3,5-tricarboxamide molecules self-assemble into a racemic mixture of one-dimensional P- and M-helical aggregates, followed by bundling into optically active higher-order aggregates or fibers (see picture). Copyright
- Stals, Patrick J. M.,Korevaar, Peter A.,Gillissen, Martijn A. J.,De Greef, Tom F. A.,Fitie, Carel F. C.,Sijbesma, Rint P.,Palmans, Anja R. A.,Meijer
-
supporting information
p. 11297 - 11301
(2013/01/15)
-
- Unique photoluminescence of diacetylene containing dendrimer self-assemblies: Application in positive and negative luminescence patterning
-
A series of poly(benzyl ether) dendrimers with two benzene-1,3,5- tricarboxamide (BTA) units bridged by diacetylene were synthesized. The formation of hydrogen bonds between BTA units to form the supramolecular self-assembly was confirmed by FT-IR and AFM
- Kim, Joo-Ho,Lee, Eunyoung,Jeong, Young-Hwan,Jang, Woo-Dong
-
experimental part
p. 2356 - 2363
(2012/08/29)
-
- Synthesis of new dendrimers - Trimesic acid derivatives
-
The efficient synthesis of new dendrimeric polyesters up to generation 3 that consist of 1,3,5-benzenetricarboxylic acid building blocks with potential applications in drug delivery is described. The dendrimers possess hydroxy or allyl functional groups o
- Salamończyk, Grzegorz M.
-
experimental part
p. 155 - 158
(2011/02/26)
-
- Supramolecular materials from benzene-1,3,5-tricarboxamide-based nanorods
-
Telechelic polymers end-capped or copolymerized with the benzene-1,3,5-tricarboxamide (BTA) moiety lead to supramolecular materials. The intrinsic phase segregation of BTA nanorods with an amorphous polymer such as poly(ethylene butylene) results in therm
- Roosma, Jorg,Mes, Tristan,Leclere, Philippe,Palmans, Anja R. A.,Meijer
-
p. 1120 - 1121
(2008/10/09)
-
- Amplification of chirality in benzene tricarboxamide helical supramolecular polymers
-
The chirality of benzene tricarboxamides is expressed and amplified into the helicity of self-assembled columnar aggregates according to 'sergeants and soldiers' and 'majority rules' principles; the strength of the amplification is analysed quantitatively
- Wilson, Andrew J.,Van Gestel, Jeroen,Sijbesma, Rint P.,Meijer
-
p. 4404 - 4406
(2007/10/03)
-