- Syntheses of chiral hybrid O,N-donor ligands for the investigation of lanthanide complex reactivities in direct aldol condensations
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A method for the synthesis of new chiral α/β-dimethylamino esters and β-amino ethers from (S,S)-hydrobenzoin is described. These new O,N-donor ligands are expected to prove a useful platform for exploring the relationship between the ligand structure and
- Mlynarski, Jacek,Jankowska, Joanna,Rakiel, Bartosz
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- PEGylated block copolymers containing tertiary amine side-chains cleavable via acid-labile ortho ester linkages for pH-triggered release of DNA
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A new type of acid-labile cationic copolymer consisting of a hydrophilic poly(ethylene glycol) (PEG) block and a polymethacrylamide block bearing tertiary amines linked by acid-labile ortho ester rings in side chains (PAOE), with defined chain length, had been synthesized via RAFT polymerization. The copolymers could efficiently bind and condense plasmid DNA at neutral pH into narrowly dispersed nano-scale polyplexes. The hydrolysis of ortho ester group in the side-chains of PAOE followed a distinct exocyclic mechanism and the rate of hydrolysis was much accelerated at mildly acidic pH, resulting in the accelerated disruption of polyplexes and the release of intact plasmid DNA. The three polymers were not toxic to cultured COS-7 cells as measured by MTT assay. As expected, PEG segments of the PEG-b-PAOE copolymers prevented nonspecific transfection of COS-7 cells. Once conjugated to a targeting ligand to enhance cell-specific entry, PEG-b-PAOE with its pH-triggered DNA release properties may achieve efficient intracellular delivery of DNA or other nucleic acid therapeutics.
- Lai, Junping,Xu, Zhangyan,Tang, Rupei,Ji, Weihang,Wang, Rui,Wang, Jun,Wang, Chun
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- Synthesis and characterization of homopolymers bearing acid-cleavable cationic side-chains for ph-modulated release of DNA
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A new type of homopolymers, PMAOE, bearing acid-cleavable cationic side-chains is synthesized and characterized. PMAOE is obtained via free radical polymerization, and they could efficiently bind and condense plasmid DNA at neutral pH. The strength of DNA binding is dependent on the length of PMAOE chains. NMR analysis reveals that hydrolysis of the ortho ester group of PMAOE follows an exocyclic mechanism and the rate of hydrolysis is much accelerated at mildly acidic pH, leading to accelerated disruption of polyplexes and release of DNA in mildly acidic environment. PMAOE is not toxic to cultured NIH 3T3 and COS-7 cells measured by MTT. This study demonstrates a unique mechanism of achieving pH-modulated binding and release of DNA from polymers with potential applications for gene delivery. A new mechanism of pH-modulated release of DNA from polymeric carrier (PMAOE) through a combination of cationic side-chain cleavage with increased polymer hydrophilicity and neutralization of residual cationic charges is demonstrated. These structurally simple side-chain degradable PMAOE homopolymers may have great potential as gene delivery vectors capable of releasing DNA in response to external or intracellular pH environment.
- Xu, Zhangyan,Lai, Junping,Tang, Rupei,Ji, Weihang,Wang, Rui,Wang, Jun,Wang, Chun
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- QUINAZOLINE DERIVATIVE AND USE THEREOF
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The present invention relates to a series of quinazoline compounds, especially compounds as represented by formula (I), isomers thereof or pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and use thereof as Pan-HER tyrosine kinase inhibitors.
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Paragraph 0284-0286
(2020/11/26)
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- Method for synthesizing 4 - (2 - (N, N - dimethylamino) ethyl) morpholine (by machine translation)
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The invention discloses a synthesis 4 - (2 - (N. The process. N- dimethylamino) ethyl) morpholine. Belong to fine chemical industry technical field. The technical scheme is: taking toluene as a solvent, N, N - dimethylethanolamine and p-toluenesulfonic acid under 110~120 °C heating reflux to carry out esterification reaction, and N, N - dimethylethanolamine p tosylate; N, N - dimethylethanolamine on tosylate reacts with morpholine, and the resulting reaction mixture is subjected to rectification to obtain a pure product. The method is cheap and easily available in raw materials, simple, mild, mild in reaction conditions, simple, high in yield, reusable, and capable of reducing cost. It is important that reaction process does not produce strong irritant gas, has reduced operating workman's health hazard greatly, does not need special corrosion-resistant equipment simultaneously, is favorable to the industrial production. (by machine translation)
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Paragraph 0028-0030; 0035-0037
(2019/10/01)
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- Synthesis, cytotoxicity, DNA binding and topoisomerase II inhibition of cassiarin A derivatives
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Four series of cassiarin A derivatives with alkanoyl (3a-3d), aroyl (4a-4d), hydroxy/amino-substituted ethylene glycol (5a-5c) and selenium-containing (6a) side chains were synthesized. Their antitumor activities were evaluated against BT474, CHAGO, HepG2
- Luesakul, Urarika,Palaga, Tanapat,Krusong, Kuakarun,Ngamrojanavanich, Nattaya,Vilaivan, Tirayut,Puthong, Songchan,Muangsin, Nongnuj
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supporting information
p. 2845 - 2850
(2014/06/10)
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- PROCESS FOR PRODUCING ORGANOLITHIUM COMPOUND AND PROCESS FOR PRODUCING SUBSTITUTED AROMATIC COMPOUND
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A method for producing an organolithium compound includes the step of reacting an aromatic compound or a halogenated unsaturated aliphatic compound and a lithiating agent in the presence of a coordinating compound containing three or more elements having a coordinating ability in a molecule, at least one thereof being a nitrogen element, or a coordinating compound containing three or more oxygen elements having a coordinating ability in a molecule, at least one of the groups containing the oxygen elements having a coordinating ability being a tertiary alkoxy group, at a temperature of ?40° C. to 40° C.
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Page/Page column 15-16
(2011/10/04)
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- NOVEL INHIBITORS OF BETA-LACTAMASE
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A class of 7-oxo-2,6-diazabicyclo-[3.2.0]-heptane-6-sulfonic acid compounds substituted at the two position of the bicyclic ring with a heterocyclylaminocarbonyl group or a carbocyclylaminocarbonyl group are β-lactamase inhibitors. The compounds and their prodrugs and pharmaceutically acceptable salts are useful in the treatment of bacterial infections in combination with β-lactam antibiotics. In particular, the compounds are suitable for use with β-lactam antibiotics (e.g., imipenem and ceftazidime) against micro-organisms resistant to β-lactam antibiotics due to the presence of the β-lactamases.
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Page/Page column 45
(2008/06/13)
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- Cyclopentadiene compound substituted with a hetero atom-containing group
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Polysubstituted cyclopentadiene-containing compound, in which at least one substituent is has the formula -RDR'n, in which R is a linking group between the cyclopentadiene and the DR'ngroup, D is a hetero atom selected from group 15 or 16 of the Periodic
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